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A BET bromodomain inhibitor that can be used for the treatment of hematologic malignancies. It binds BET proteins to suppress the interaction between these proteins, propeins and acetylated chromatin, as well as transcription factors. The BET bromodomain inhibitor modulates the expression of oncogenes. Uses: The treatment of hematologic malignancies. Synonyms: MDK3597; MDK-3597; MDK 3597; BET bromodomain inhibitor. 2-[8-Chloro-6-(4-chloro-phenyl)-1-methyl-4H-3-oxa-2,5-diaza-benzo[e]azulen-4-yl]-acetamide. Grade: ≥98%. CAS No. 1505453-59-7. Molecular formula: C20H15Cl2N3O2. Mole weight: 400.259.
BET bromodomain inhibitor
BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11. Uses: Scientific research. Group: Signaling pathways. CAS No. 1505453-59-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-103036.
BET bromodomain inhibitor 1
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor (IC50 = 2.6 nM for BRD4) with anticancer activity. It binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2) and BRDT(2) with high affinities (Kds of 1.3, 1.0, 3.0, 1.6 and 2.1 nM, respectively). Synonyms: Pyrrolo[1,2-a]pyrazin-1(2H)-one, 6-[2-(2,4-difluorophenoxy)-5-[(ethylsulfonyl)methyl]-3-pyridinyl]-8-methyl-. Grade: ≥95%. CAS No. 2411226-02-1. Molecular formula: C22H19F2N3O4S. Mole weight: 459.47.
BET bromodomain inhibitor 3
BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with K i value of > 40 μM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 854137-39-6. Pack Sizes: 10 mg. Product ID: HY-153593.
BET bromodomain inhibitor 4
BET bromodomain inhibitor 4 (example 7) is an inhibitor of the BET bromodomain domain [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2407658-41-5. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-157393.
2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide is an effective BET bromodomain inhibitor with an IC50 of 37 nM for BRD4. Synonyms: 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-2,3,9-trimethyl-; 4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide; CPI 203 (rac isomer). Grade: ≥95%. CAS No. 202591-23-9. Molecular formula: C19H18ClN5OS. Mole weight: 399.90.
3-Bromo-5-hydroxybenzyl Alcohol
3-Bromo-5-hydroxybenzyl Alcohol is an intermediate used to prepare (isoxazolylphenyl) arylmethanols as inhibitors of the BET bromodomain family member BRD4(1) for potential use as antitumor agents. Group: Biochemicals. Grades: Highly Purified. CAS No. 1020336-51-9. Pack Sizes: 500mg, 1g. Molecular Formula: C7H7BrO2, Molecular Weight: 203.03. US Biological Life Sciences.
Worldwide
ABBV-744
ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers. Synonyms: N-ethyl-4-(2-(4-fluoro-2,6-dimethylphenoxy)-5-(2-hydroxypropan-2-yl)phenyl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide. Grade: ≥98%. CAS No. 2138861-99-9. Molecular formula: C28H30FN3O4. Mole weight: 491.55.
Alobresib
Alobresib is a novel BET bromodomain inhibitor. Alobresib reversibly binds the BET bromodomain proteins BRD2, BRD3, BRD4, and BRDT and prevents protein-protein interaction between BET proteins and acetylated histones and transcription factors, against multiple primary USC cell lines overexpressing c-Myc. Synonyms: GS-5829. CAS No. 1637771-14-2. Molecular formula: C26H23N5O2. Mole weight: 437.49.
Apabetalone
Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC 50 s are 87 μM and 0.51 μM for BD1 and BD2 , respectively [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: RVX-208; RVX000222. CAS No. 1044870-39-4. Pack Sizes: 10 mM * 1 mL; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-16652.
AZD5153
AZD5153 (Compound 13) is a trivalent triazolpyrazine bromide domain (BRD), bromodomain and extraterminal (BET) inhibitor. AZD5153 has down-regulated c-Myc gene and tumor growth inhibition activity. AZD5153 can be used in the study of BET small molecule inhibitors [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1869912-39-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg. Product ID: HY-100653.
AZD 5153
AZD5153 is a potent, selective, and orally available inhibitor of the bromodomain and extraterminal (BET). It can simultaneously bind two bromodomains in BRD4 with the IC50 value of 5 nM, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma. AZD5153 also shows enhanced potency as a result of bivalent binding and a clear correlation between BRD4 activity and cellular potency. Synonyms: AZD-5153; AZD5153; (R)-4-(2-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-one. Grade: 98%. CAS No. 1869912-39-9. Molecular formula: C25H33N7O3. Mole weight: 479.57.
AZD5153 6-Hydroxy-2-naphthoic acid
AZD5153 6-Hydroxy-2-naphthoic acid, a 6-hydroxy-2-naphthoic acid salt of AZD-5153, is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor possessing a bivalent binding mode (pKi = 8.3 for BRD4). Synonyms: AZD5153 6-Hydroxy-2-naphthoic acid; AZD 5153 6-Hydroxy-2-naphthoic acid; AZD-5153 6-Hydroxy-2-naphthoic acid; 6-hydroxynaphthalene-2-carboxylic acid; 4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-1,3-dimethylpiperazin-2-one. CAS No. 1869912-40-2. Molecular formula: C36H41N7O6. Mole weight: 667.75.
AZD5153 6-Hydroxy-2-naphthoic acid
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC 50 of 1.7 nM. Uses: Scientific research. Group: Signaling pathways. CAS No. 1869912-40-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-100653A.
BET-IN-1
BET-IN-1, an oxazole derivative, can be used as a bromodomain inhibitor. Synonyms: 4-[8-methoxy-1-[(2R)-1-methoxypropan-2-yl]-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazoleBET-IN-1; BET IN 1SCHEMBL14698278CS-5464; HY-19760; CS 5464; HY 19760; CS5464; HY19760. CAS No. 1422554-34-4. Molecular formula: C25H30N4O4. Mole weight: 450.53.
BI-9564
BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 ?M and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 ?M for BET family[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1883429-22-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-100352.
BMS-986158
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins with potential antineoplastic activity. Synonyms: 2-[3-(3,5-dimethyltriazol-4-yl)-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol; BMS-986158; BMS 986158; BMS986158. CAS No. 1800340-40-2. Molecular formula: C30H33N5O2. Mole weight: 495.62.
Bromodomain inhibitor-8
Bromodomain inhibitor-8 is a BET bromodomain inhibitor used for the treatment of autoimmune and inflammatory diseases. Synonyms: Benzoic acid, 4-[(2S,4R)-1-acetyl-4-[(4-chlorophenyl)amino]-1,2,3,4-tetrahydro-2-methyl-6-quinolinyl]-, methyl ester; Methyl 4-{(2S,4R)-1-acetyl-4-[(4-chlorophenyl)amino]-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl}benzoate. Grade: ≥98%. CAS No. 1300031-70-2. Molecular formula: C26H25ClN2O3. Mole weight: 448.94.
CD161
CD161 is a potent, selective and orally active BET bromodomain inhibitor with Ki values of 8.2 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. In human leukemia cell lines MV4-11 and MOLM-13, CD161 strongly inhibits cell growth and induces apoptosis, with IC50s <100 nM. Synonyms: CD-161; CD 161; 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole. Grade: 98%. CAS No. 1627716-22-6. Molecular formula: C26H21N5O2. Mole weight: 435.48.
CD235
CD235 is a structurally similar analogue of CD161, which is a potent and orally bioavailable inhibitor of BET bromodomain. Synonyms: 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-4-(6-fluoro-4-quinolinyl)-6-methoxy-2-methyl-9H-pyrimido[4,5-b]indole; 9H-Pyrimido[4,5-b]indole, 7-(3,5-dimethyl-4-isoxazolyl)-4-(6-fluoro-4-quinolinyl)-6-methoxy-2-methyl-. Grade: ≥95%. CAS No. 1627716-57-7. Molecular formula: C26H20FN5O2. Mole weight: 453.47.
CF53
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K i of <1 nM, K d of 2.2 nM and an IC 50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1808160-52-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-112610.
CF53
CF53 is a selective, highly potent and orally active BET protein inhibitor, with a Ki of <1 nM, Kd of 2.2 nM and IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. It has potent antitumor activity in vitro and in vivo. Synonyms: N-(3-Cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-2-methyl-9H-pyrimido[4,5-b]indol-4-amine; BET inhibitor CF53; 9H-Pyrimido[4,5-b]indol-4-amine, N-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethyl-4-isoxazolyl)-6-methoxy-2-methyl-; CF53 free base. Grade: ≥98%. CAS No. 1808160-52-2. Molecular formula: C24H25N7O2. Mole weight: 443.50.
CPI203
CPI203, also known as TEN010, JQ-2; RO6870810 and RG6146, is a potent and orally active BET bromodomain inhibitor. CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. CPI203 ownregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. CPI203 arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). Uses: Designed for use in research and industrial production. Additional or Alternative Names: CPI203; CPI-203; CPI 203; TEN010; TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RG 6146; RG-6146; RO6870810; RO-6870810; RO 6870810. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1446144-04-2. Molecular formula: C19H18ClN5OS. Mole weight: 399.9. Purity: >98%. IUPACName: (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide. Canonical SMILES: O=C(N)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1. Product ID: ACM1446144042. Alfa Chemistry ISO 9001:2015 Certified.
CPI-203
CPI-203 is a BET bromodomain inhibitor. It inhibits BRD4 in vitro and in cells, and causes G1 cell cycle arrest. It also arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). Synonyms: CPI203; CPI-203; CPI 203; TEN010; TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RG 6146; RG-6146; RO6870810; RO-6870810; RO 6870810. (6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide. Grade: >98%. CAS No. 1446144-04-2. Molecular formula: C19H18ClN5OS. Mole weight: 399.90.
CPI-203
CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 ?-screen assay). Uses: Scientific research. Group: Signaling pathways. CAS No. 1446144-04-2. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-15846.
CPI-637
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively. CPI-637 displayed a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50=11.0 ± 0.6 μM). Synonyms: CPI-637; CPI 637; CPI637. (4R)-4-methyl-6-[1-methyl-3-(1-methylpyrazol-4-yl)indazol-5-yl]-1,3,4,5-tetrahydro-1,5-benzodiazepin-2-one; CPI-637; SCHEMBL17673230. Grade: >98%. CAS No. 1884712-47-3. Molecular formula: C22H22N6O. Mole weight: 386.459.
FT001
FT001 is a potent, selective and orally effective BET Bromodomain inhibitor with antitumor activity. FT001 inhibits MYC expression with an IC50 of 0.46 μM. FT001 has an effective anti-proliferation effect on MV-4-11, showing obvious MYC mRNA inhibition both in vitro and in vivo. Synonyms: (S)-1-(4-(cyclopropanecarbonyl)-6-(4-(1,1-dioxidothiomorpholino)phenyl)-2-methyl-3,4-dihydroquinoxalin-1(2H)-yl)ethan-1-one; Ethanone, 1-[(2S)-4-(cyclopropylcarbonyl)-6-[4-(1,1-dioxido-4-thiomorpholinyl)phenyl]-3,4-dihydro-2-methyl-1(2H)-quinoxalinyl]-; FT001; FT-001; 1-[(2S)-4-(Cyclopropylcarbonyl)-6-[4-(1,1-dioxido-4-thiomorpholinyl)phenyl]-3,4-dihydro-2-methyl-1(2H)-quinoxalinyl]ethanone. Grade: ≥95%. CAS No. 1778655-51-8. Molecular formula: C25H29N3O4S. Mole weight: 467.58.
GSK046
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity[1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: iBET-BD2. CAS No. 2474876-09-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136571.
GSK097
GSK097, a potent and selective inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins, shows 2000-fold selectivity for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media. Synonyms: 2,4-Pyridinedicarboxamide, 6-[(S)-hydroxyphenylmethyl]-N2-methyl-N4-[(1S,2S)-2-methylcyclopropyl]-. CAS No. 2159137-02-5. Molecular formula: C19H21N3O3. Mole weight: 339.39.
GSK525762
GSK525762A, also known as I-BET-762 and GSK525762, is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity. Upon administration, the BET inhibitor GSK525762 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, BET proteins, comprising of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth. Synonyms: GSK525762; GSK525762; GSK525762; GSK525762A; GSK-525762A; GSK 525762A; I-BET-762; I-BET762; I-BET 762; molibresib. CAS No. 1260907-17-2. Molecular formula: C22H22ClN5O2. Mole weight: 423.9.
GSK 525768A
GSK 525768A is a enantiomer analogue of GSK 525762A which is a BET family inhibitor aiming at the bromodomain and has potential effect against cancers and sorts of other diseases related to BET bromodomains. Uses: Gsk 525768a is a enantiomer analogue of gsk 525762a which is a bet family inhibitor aiming at the bromodomain and has potential effect against cancers and sorts of other diseases related to bet bromodomains. Synonyms: GSK 525768A; GSK525768A; GSK-525762A; CHEMBL2153435; SCHEMBL12966358; DTXSID50680634. Grade: 98%. CAS No. 1260530-25-3. Molecular formula: C22H22ClN5O2. Mole weight: 423.90.
GSK5959
GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 value of 80 nM. It exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. It is used at 10 μM final concentration in various in vitro assays. It disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3 in vitro. Uses: Gsk-5959 disrupts chromatin binding of brpf1 in a cellular assay. Synonyms: N-(1,3-dimethyl-2-oxo-6-piperidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide; GSK-5959; GSK 5959; GSK5959. Grade: >98%. CAS No. 901245-65-6. Molecular formula: C22H26N4O3. Mole weight: 394.47.
GSK620
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2088410-46-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-137892.
GSK778
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[1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: iBET-BD1. CAS No. 2451862-42-1. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136570.
GSK778
GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. Synonyms: GSK-778; GSK 778; iBET-BD1. Grade: 99%. CAS No. 2451862-42-1. Molecular formula: C30H33N5O3. Mole weight: 511.63.
GW841819X
GW841819X, a benzodiazepin derivative, has been found to be a BET bromodomains inhibitor that could be probably significant in the study of myeloma and leukemia at some extent. Synonyms: KB-75882; KB 75882; KB75882; benzyl (1-methyl-6-phenyl-4hbenzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)carbamate. Grade: 98%. CAS No. 146135-18-4. Molecular formula: C25H21N5O2. Mole weight: 423.48.
I-BET151
I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4 , BRD2 , and BRD3 with pIC 50 of 6.1, 6.3, and 6.6, respectively [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: GSK1210151A. CAS No. 1300031-49-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13235.
I-BET151
I-BET151 is a BET bromodomain inhibitor, which blocks recruitment of BET to chromatin. It was shown to induce early cell cycle arrest and apoptosis in human and mouse MLL-fusion leukemia cell lines. Synonyms: GSK1210151A; 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one. Grade: >98%. CAS No. 1300031-49-5. Molecular formula: C23H21N5O3. Mole weight: 415.453.
I-BET 151 dihydrochloride
The hydrochloride salt form of I-BET 151, which has been found to be a BET bromodomain inhibitor and exhibit activities against human and murine MLL-fusion leukaemic cell lines. Synonyms: I-BET 151 dihydrochloride; I BET 151 dihydrochloride; IBET 151 dihydrochloride; IBET151 dihydrochloride; 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydroxy-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one dihydrochloride. Grade: ≥98% by HPLC. CAS No. 1883545-47-8. Molecular formula: C23H21N5O3.2HCl. Mole weight: 488.37.
Isoxazole
Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor? [1] [2] [3] [4] [5]. Uses: Scientific research. Group: Signaling pathways. CAS No. 288-14-2. Pack Sizes: 10 mM * 1 mL; 25 g; 50 g. Product ID: HY-W010649.
(+)-JQ-1
BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. Group: Biochemicals. Alternative Names: (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic Acid 1,1-Dimethylethyl Ester; (+)-JQ1; (S)-(+)-Tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate. Grades: Highly Purified. CAS No. 1268524-70-4. Pack Sizes: 5mg, 10mg, 25mg, 50mg, 100mg. Molecular Formula: C??H??ClN?O?S, Molecular Weight: 456.99. US Biological Life Sciences.
Worldwide
(+)-JQ-1
(+)-JQ-1 is a potent and selective BET bromodomain inhibitor, IC50 values are 77 nM and 33 nM for inhibiting BRD4 (N-terminal) and BRD4 (C-terminal), respectively. Synonyms: JQ1. CAS No. 1268524-70-4. Molecular formula: C23H25ClN4O2S. Mole weight: 456.99.
(+)-JQ-1
(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))[1]. (+)-JQ-1 also activates autophagy[2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: JQ1. CAS No. 1268524-70-4. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 50 mg; 100 mg; 500 mg. Product ID: HY-13030.
JQ-1 (carboxylic acid)
JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4. Uses: Scientific research. Group: Signaling pathways. CAS No. 202592-23-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg. Product ID: HY-78695.
(+)-JQ1 PA
(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM. (+)-JQ1 PA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Uses: Scientific research. Group: Signaling pathways. CAS No. 2115701-93-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112789.
Mivebresib
Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a K i of 1.5 nM [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ABBV-075. CAS No. 1445993-26-9. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-100015.
Molibresib
Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC 50 of 32.5-42.5 nM. Uses: Scientific research. Group: Signaling pathways. Alternative Names: I-BET762; GSK525762; GSK525762A. CAS No. 1260907-17-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-13032.
NEO2734
NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains[1]. NEO2734 is active in SPOP mutant and wild-type prostate cancer[2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: EP31670. CAS No. 2081072-29-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136938.
NVS-CECR2-1
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 ( CECR2 ) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity ( IC 50 =47 nM; K D =80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1992047-61-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-110374.
ODM-207
ODM-207 (BET-IN-4) is a potent BET bromodomain protein ( BRD4 ) inhibitor, with an IC 50 of ≤ 1 μM [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BET-IN-4. CAS No. 1801503-93-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-111916.
PFI-1
PFI-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs with acetylated histone tails. Co-crystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts. Uses: Designed for use in research and industrial production. Additional or Alternative Names: PFI1; PFI 1; PFI-1. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1403764-72-6. Molecular formula: C16H17N3O4S. Mole weight: 347.39. Purity: >98%. IUPACName: 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide. Canonical SMILES: O=S(C1=CC=CC=C1OC)(NC2=CC3=C(NC(N(C)C3)=O)C=C2)=O. Product ID: ACM1403764726. Alfa Chemistry ISO 9001:2015 Certified. Categories: PFM-1 mine.
PLX51107
PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range). Uses: Scientific research. Group: Signaling pathways. CAS No. 1627929-55-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-111422.
PPI Inhibitor Library
A unique collection of 260 PPI-related compounds for drug screening; - Targets include PD-1/PD-L1, Bcl-2, BET bromodomain, BRD4 bromodomain, etc. - Detailed compound information with structure, target, and biological activity description; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L9400. Categories: PPI Inhibitor Libraries.
(R)-(-)-JQ1
(R)-(-)-JQ1 is the R-isomer and an inactive control of JQ1, a BET bromodomain inhibitor. Synonyms: (-)-JQ1; (-)-JQ 1; (-)-JQ-1; (R)-JQ1; (R)-(-)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate. Grade: >95%. CAS No. 1268524-71-5. Molecular formula: C23H25ClN4O2S. Mole weight: 456.989.
RVX-297
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 ?M for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1044871-04-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-114504.
JQ1 Enantiomers Set ((S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate, SGCBD01, BRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I)
A cell-permeable I-BET class of thienodiazepine derivative whose (S)-(+), but not (R)-(-), enantiomer is shown to target both bromodomains (BD1 & BD2) of BET family members BRD2, BRD3, BRD4, and BRD6/BRDT in a Kac- (epsilon-N-acetylated lysine) competitive manner, exhibiting little affinity toward 23 other BD-containing proteins, BRD1 and BRD9, and little or no activity against a panel of more than 50 receptors, ion channels, and transporters. Effectively inhibits the oncogenic BRD4-NUT fusion-dependent NUT midline carcinoma and c-Myc oncoprotein-dependent multiple myeloma proliferation both in cultures (IC50 <1uM) in vitro and in mice (50mg/kg/day i.p.) in vivo. Also reported to cross the blood-testis boundary in male mice and effectively block BRDT-mediated spermatogenesis without affecting hormone levels. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1set. US Biological Life Sciences.
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