≥98% (HPLC)GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Applications Products Services Documents Support. GSK778 phenocopies the. GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 Hydrochloride. Email. *. The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. We do not sell to patients. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. 09-Sep-2023. They are useful assets for example, in phenotypic assays, or as a starting point for medicinal chemistry campaigns. Applications Products Services Documents Support. GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). 451491-47-7 CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells. Safety Information. Email. 5 gsk778 (pan-bd2) ↓mcp-1 in lps-stimulated pbmcs: 1000 <10 gsk791 32193360 6 brd: baz2a/2b baz2-icr frap, baz2a: 1000 1 - 25719566 7 gsk2801 frap, baz2b: 1000 3 gsk8573 25799074 8 brd: brd9/7 bi-9564 frap, brd9/7: 100/1000 1 - 26914985 9 tp-472 nanobret, brd9: 323 (ec 50) 1 tp-472n 10 brd: brd9 i-brd9 nanobret, brd9: 159 1 - 25856009 11 brd. 7 B) indicated that GSK778 maintains all of the critical interactions of I-BET151 with BRD4-BD1, including the hydrogen bonding interaction of the 3,5-dimethylisoxazole moiety with the conserved Asn140, the hydrophobic interaction of the aryl ring of the α-methylbenzyl group with the. Theoretical Analysis Hodoodo Cat#: H408120 Name: GSK778 CAS#: 2451862-42-1By surface plasmon resonance binding assay, GSK778 is > 130-fold selective for BD1, whereas GSK046 is > 300-fold selective for BD2 [26]. Applications Products Services Documents Support. The addition of olinone to oligodendrocyte progenitor cells demonstrated biological effects divergent from pan-BET inhibition. Available to order from Sigma-Aldrich. Resolution:A concentration of 1-2 µM of I-BET151, GSK778, GSK789, or GSK046 was used for cell culture treatments as recommended by our collaborators at GlaxoSmithKline (54–56). Copy Link. Email. GSK778 phenocopies the effects of pan- BET inhibitors in cancer models. All Photos (1) SML3234. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. ChemicalBook provide Chemical industry users with GSK778 Boiling point Melting point,GSK778 Density MSDS Formula Use,If You also need to GSK778 Other information,welcome to contact us. In addition, while GSK778 phenocopied I-BET151 in terms of antiproliferative effects on a range of human cancer cells, GSK046 was less effective. MS EN. ≥98% (HPLC)Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 14 GSK778, another pan-D1-selective inhibitor (Figure 1A), was recently reported. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. (A) Schematic of the BET Bromodomain proteins and chemical structures. All Photos (1) SML3234. HK EN. Comprar GSK778 hydrochloride na CymitQuimica a partir de 181,0 € Iniciar Sessão Criar uma conta. Particularly, GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells. GSK778 Hydrochloride. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. 1 μg/mL, which we determined was the equivalent of 1000 units/mL (U/mL) via in-house. FRAP, BAZ2B: 1000 3:. The. As epigenetic readers, bromodomain and extra-terminal domain (BET) family proteins bind to acetylated-lysine residues in histones and recruit protein complexes to promote transcription initiation and elongation. gov or . Molecular Formula: C30H33N5O3. BET BD1 related products. ≥98% (HPLC)Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. Solubility: Soluble in DMSO. 4. 11 - Combustible Solids. All Photos (1) Documents. GSK778 hydrochloride | C30H34ClN5O3 | CID 168013350 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046, affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to. S1F, and table S1). SML3234. Fax: +1 510. Data and materials availability: I-BET151, GSK778, GSK046, and GSK620 are available from R. GSK778 Hydrochloride. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. GB EN. 10 µM; GSK791. GSK789 was derived from a series of naphthyridone ATAD2 inhibitors. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Buy Epigenetic Reader Domain inhibitor GSK778 (iBET-BD1) from AbMole BioScience. The . GSK778. SML3234. Catalog No. R (moc. 5 upper limit of normal (ULN) Total bilirubin < 1. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GuHCl may be used in understanding the circular dichroism of many polypeptides and proteins. ABBV-744 is highly selective for BD2 of BRD2, BRD3 and BRD4, 64 exhibiting several hundred-fold higher affinity for the BD2 over BD1. WGK. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Cell lysates were separated by SDS-PAGE on [email protected] μg/mL, which we determined was the equivalent of 1000 units/mL (U/mL) via in-house. S1F, and table S1). Available to order from Sigma-Aldrich. Additionally, while GSK778 phenocopied I-BET151 in terms of anti-proliferative effects on a range of human cancer cells, GSK046 was less effective. This was explained by displacement of BET proteins from promoter and enhancer regions that control MYC expression, suggest-ing that BD1 anchors BET. Sigma-Aldrich. Catalog Number: AA01KEG7. Please continue to check back for new reviews and commentary. iBET-BD1 phenocopies the effects of pan-BET inhibitors in cancer models, whereas iBET-BD2 is predominantly effective in. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. All Photos (1) Documents. Available to order from Sigma-Aldrich. Recent clinical studies have shown that BRD4 expression in glioma is significantly higher than in the adjacent normal brain tissue. Email. The authors found that in mouse models of various cancers, BD1 inhibition is. Related Post. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. 27,42 The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. their selectivity. GSK778 Hydrochloride. Preis und Verfügbarkeit anzeigen. Hazard Description: Toxic. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. thesgc. Available to order from Sigma-Aldrich. The bromodomain (BD) is a ~110 amino acid motif that binds to acetyl-lysine modifications on histone and non-histone proteins (Dhalluin et al. SML3168. COO/ COA. 6SWN, 6SWO, 6SWP, 6SWQ. The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes. In addition, recent studies have shown that selective. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. WGK 3. Herein,. GSK778 Hydrochloride. Guanidine hydrochloride; Useful for denaturing proteins and solubilization of inclusion bodies. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Adequate renal, hepatic, pulmonary and cardiac function defined as: Creatinine clearance (as estimated by Cockcroft Gault) > 60 mL/min. GSK778. comThe calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. All Photos (1) SML3234. However, distinct from BD1-selective and pan-BET inhibitors, the BD2. VN EN. Probe criteria. Available to order from Sigma-Aldrich. Endoplasmic Reticulum Stress Modulator (ERSM) Epigenetics Resch Products. Le GSK778 montre également de forts effets anti-cancéreux in vivo, prolongeant la survie de souris atteintes de leucémies myéloïdes aiguë [422, 423]. ≥98% (HPLC)GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 53 reported the development route of iBET-BD1 from a pan-BET imidazoquinolinone-based inhibitor with a slight BD1-bias, iBET151. Email. Applications Products Services Documents Support. Contains a pharmaceutically active ingredient. GSK778 Hydrochloride. Find here details of companies selling GSK778, for your purchase requirements. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. AR EN. Herein, GSK778 and GSK046 are referred to as iBET-BD1 and iBET-BD2, respectively. CPI-0610 is another second-generation BET inhibitor with a molecular structure similar. GSK778. COO/ COA. Copy Link. Available to order from Sigma-Aldrich. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. CAS# 2451862-42-1. IQ EN. Chemical probes are cell-active, selective, highly validated research tools that can be used to decipher the biology of their target. If not otherwise indicated, cells were pretreated with I-BET151, iBET-BD1, iBET-BD2 or vehicle (DMSO) for 48 hours, irradiated with 0 or 6 Gy, and incubated for additional time intervals with concurrent drug. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. gov means it’s official. 2h 04m. To explore the individual functional. Saturday. ChemScene Provide GSK778(CAS 2451862-42-1)In-stock or Backordered impurities,Bulk custom synthesis,Formular C30H33N5O3,MW 511. Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. All Photos (1) Documents. , 2019). 6 GSK789 (BD1) IC50= 125 nM (MV-4−11 cells) <10: GSK791. COO/ COA. $79. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Phylogenetic tree of the human bromodomain-containing protein subgroups. 00. orgGSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. * Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients. Figure 4. Available to order from Sigma-Aldrich. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. Solubility: Soluble in DMSO. BRD4. Copy Link. All Photos (1) Documents. Email. Apart from BRDs, YEATS family members have been. GSK778 Hydrochloride. SML3234. GM6001. described the development of GSK778 (iBET-BD1) and GSK046 (iBET-BD2), the first highly selective small-molecule inhibitors of BET-BD1 and BET-BD2, respectively . ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. Applications Products Services Documents Support. , 2013). Catalog No. 포함:구조식 이미지,카스 번호(CAS),분자식,녹는점,끓는 점,밀도. 5 (LPS-PBMC assay) <10: 8 GSK620 (BD2) pIC50 = 7. 5 (LPS-PBMC assay) ≤ 10 µM. Solubility: Soluble in DMSO. Despite their profound preclinical efficacy, the clinical utility of pan-inhibitors is limited due to observed cytotoxicicities. Products are for research use only. The two tandem bromodomains of the BET proteins enable chromatin binding to facilitate transcription. GSK778 hydrochloride | C30H34ClN5O3 | CID 168013350 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological. Inhibitor/agonist potency: goal is < 50 nM (IC 50, K D) Surpasses criterion: :BET mutant TR-FRET assay: BRD2 (BD1) pIC 50 = 7. SML3234. Catalog Number: AA01KEG7. GSK778 (iBET-BD1) [GSK reference 1, 5] is an analogue of I-BET151 [68] with good potency against BET BD1s (IC 50 s ≈ 40–75 nM) and similar selectivity to LT052 between the BDs of BRD4 (110-fold -to 140-fold depending on assay format), but this selectivity is slightly lower for BRD2 and BRD3 (30–65-fold). ChemicalBook あなたのためにGSK778(2451862-42-1)の化学的性質を提供して、融点、価格、蒸気圧、沸点、毒性、比重、沸点、密度、分子式、分子量、物理的な性質、毒性 税関のコードなどの情報、同時にあなたは更にGSK778(2451862-42-1)の製品の全世界の供給商にブラウズすることができて、生産企業と生産. Safety Information. Given the high sequence similarity amongst BET bromodomains, small molecule inhibitors for a single BET bromodomain are lacking; however, potent pan-D2 inhibitors (e. GM6001. HY-136570 25mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. ID EN. A concentration of 1-2 µM of I-BET151, GSK778, GSK789, or GSK046 was used for cell culture treatments as recommended by our collaborators at GlaxoSmithKline (54–56). GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Email. Applications Products Services Documents Support. COO/ COA. WGK. 61: Molecular Formula: C 30 H 33 N 5 O 3. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. Europe PMC is an archive of life sciences journal literature. SML3234. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. ([email protected]) under a material transfer agreement with GSK. 00. S9683 Synonyms: iBET-BD1. Available to order from Sigma-Aldrich. Les inhibiteurs spécifiques du. Email. On the basis of sequence homology, BCPs are classified into eight different subgroups (families). GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. ≥98% (HPLC)GSK778 ( iBET-BD1 ) Catalog No. SML3234. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Email. 2451862-42-1: GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively; GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 Hydrochloride. INTRODUCTION. However, many compounds reported in the literature and routinely. GSK778 phenocopies the. A panel of biocatalytic systems was tested to identify biocatalysts suitable for milligram scale production of metabolite M4. SA EN. ≥98% (HPLC)Shop Medchemexpress LLC HY-136570 5mg , GSK778 CAS:2451862-42-1 Purity:>98% at Fishersci. They are epigenetic readers of histone acetylation with broad specificity. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 999. GSK778 Hydrochloride. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. g ABBV-744, Fig. Safety Information. Sigma-Aldrich. ksg@ahjnirp. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778, a potent pan-D1 inhibitor, was reported by Gilan et al. GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. This advance has helped to highlight more distinct roles of BD1 and BD2 ( Figure 5 ). GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. COO/ COA. Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). IL EN. Applications Products Services Documents Support. BRD4 inhibitors effectively penetrate the blood-brain barrier and target glioma tumor tissues but have little effect on normal brain tissues. Applications Products Services Documents Support. Some, such as ABBV-744 and GSK778, are optimized for greater selectivity for one of two distinct BET protein bromodomains in an effort to improve therapeutic indices [55, 56]. KR EN. Applications Products Services Documents Support. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification codes 6SWN, 6SWO, 6SWP, and 6SWQ. Available to order from Sigma-Aldrich. All Photos (1) Documents. COO/ COA. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis . GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. ksg@ahjnirp. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 999. ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. 5. HY-136570 10mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. ≥98% (HPLC) All Photos (1)GSK778 (iBET-BD1) هو مثبط قوي وانتقائي BD1 bromodomain لبروتينات BET ، مع IC50s 75 نانومتر (BRD2 BD1) ، 41 نانومتر (BRD3 BD1) ، 41 نانومتر (BRD4 BD1) ، و 143 نانومتر (BRDT BD1) ، على التوالى. All Photos (1) Documents. EG EN. 5 upper limit of normal (ULN) Total bilirubin < 1. GSK778. Copy Link. SML3234. GSK778 Hydrochloride. Safety Information. BET proteins are linked to cancer progression due to their. Pan-BD1 inhibitors (which have higher inhibitory activity for BD1 than BD2 of BET proteins) are comparable to pan-BD inhibitors, such as MS436, 59 Olinone, 60 MS402, 61 3U, 62 GSK778, 19 ZL0516. WGK 3. IC₅₀ & Target BRD2 BD1 75 nM (IC50) BRD3 BD1 41 nM. This approach Product Description. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. Available to order from Sigma-Aldrich. Available to order from Sigma-Aldrich. S1F, and table S1). 6swo: c-terminal bromodomain of human brd2 with ibet-bd1 (gsk778)BRD3. 65 In turn, pan-BD2 inhibitors (which have higher inhibitory activity for BD2 than BD1 of BET family members) are. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. Applications Products Services Documents Support. GSK778 Hydrochloride. A concentration of 1-2 µM of I-BET151, GSK778, GSK789, or GSK046 was used for cell culture treatments as recommended by our collaborators at GlaxoSmithKline (54–56). 11 - Combustible Solids. nM, SPR BRD4 (BD1): pKd= 8. , 2020; Gilan et al. Hazard identification. MM EN. Applications Products Services Documents Support. Applications Products Services Documents Support. 2 Relevant identified uses of the substance or mixture and uses advised against; Identified uses: For research use only, not for human or veterinary use. , 2020), and others has revealed remarkably gene-selective transcriptional defects. 00. 61: Synonym: GSK778;4-[2-(methoxymethyl)-1-[(1~{R})-1-phenylethyl]-8-[[(3~{S})-pyrrolidin-3-yl. Available to order from Sigma-Aldrich. Europe PMC is an archive of life sciences journal literature. Buy Epigenetic Reader Domain inhibitor GSK778 (iBET-BD1) from. org); (b) BET BD1-selective GSK778 bound to BRD4-BD1 (in cyan,. Phylogenetic tree of the human bromodomain-containing protein subgroups. GSK778 Hydrochloride. 11 - Combustible Solids. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains. , 2016). Copy Link. The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. The two. MOscan analysis of GSK778 indicated the binding of this compound only to BET bromodomains with strong binding to BET BD1 domains while weakly binding to BET BD2 domains. Copy Link. COO/ COA. GSK778 (iBET-BD1) ist ein potenter und selektiver BD1-BromodomÄnen-Inhibitor der BET-Proteine mit IC50-Werten von 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1) und 143 nM (BRDT BD1) , beziehungsweise. Código de clase de almacenamiento. Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections Ram K. For example, whereas a BD1-selective inhibitor (GSK778) showed similar phenocopies of pan BETis in cancers, a BD2-selective inhibitor (GSK046) showed better effectiveness in inflammatory and autoimmune diseases 2. PK EN. . Potent, selective and cell-permeable inhibitors of protein function ("chemical probes") are valued reagents in both fundamental and applied biological research, and they are essential for the early stages of drug discovery by allowing preclinical target validation in both academic and industrial laboratories. First of all, GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. GSK778 reduces the production of anti-keyhole limpet. • RVX-208 (Apabetalone), which is a BD2-selective BETi showing 30-to. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. If not otherwise indicated, cells were pretreated with I-BET151, iBET-BD1, iBET-BD2 or vehicle (DMSO) for 48 hours, irradiated with 0 or 6 Gy, and incubated for additional time intervals with concurrent drug. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。 Recently, Gilan et al. ABBV-744 is highly selective for BD2 of BRD2, BRD3 and BRD4, 64 exhibiting several hundred-fold higher affinity for the BD2 over BD1. Using these molecules, Gilan et al. Open in a separate window. All Photos (1) SML3234. ≥98% (HPLC)HY-136570 10mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 Hydrochloride. Copy Link. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains outside of. Safety Information. FRAP, BAZ2A: 1000 1-25719566: 10 GSK2801. 5. Its mechanism of action is not fully understood. Instruction. Glatiramer acetate is a mixture of synthetic peptides randomly composed of glutamic acid, lysine, alanine, and tyrosine. ≥98% (HPLC)MOscan analysis of GSK778 indicated the binding of this compound only to BET bromodomains with strong binding to BET BD1 domains while weakly binding to BET BD2 domains. MedKoo CAT#: 408120. Available to order from Sigma-Aldrich. ([email protected]) and I. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 6SWO: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH iBET-BD1 (GSK778) PDB ID: 6SWO Download: MMDB ID: 192698: PDB Deposition Date: 2019/9/22: Updated in MMDB: 2021/02: Experimental Method: x-ray diffraction. Meanwhile, GSK778 has IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively.