Cat. No. | Product Name | Target | Signaling Pathways |
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T77339 |
BRD4-IN-4
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4-IN-4 是一种具有选择性的 BRD4 抑制剂 ,对 BRD4 的IC50值为 6.83 μM。BRD4-IN-4 选择性抑制 MV4-11 细胞系增殖并将细胞阻滞在 G1 期。BRD4-IN-4可用于研究 MLL 白血病。 | |||
T40305 |
BRD4-IN-2
BRD4-IN-2 |
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BRD4-IN-2 is a bromodomain BRD4 inhibitor with an IC 50 value of 9.9 nM. | |||
T30580 |
BRD4-Kinases-IN-3
BRD4 kinases inhibitor 3,BRD4-Kinases inhibitor-3 |
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BRD4-Kinases-IN-3 is a dual BRD4-Kinases inhibitor that can be used as a value-added multi-targeted chemical probe for cancer therapy. | |||
T10521 |
ODM-207
BET-IN-4,ODM207 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
ODM-207 (BET-IN-4) 是一种 BET 溴区结构域蛋白的抑制剂,对 BRD4的 IC50值 ≤ 1 μM。 | |||
T61318 |
BRD4 Inhibitor-20
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4 Inhibitor-20是一种有效的溴结构域蛋白4(BRD4)抑制剂,具有口服活性。BRD4 Inhibitor-20在癌细胞系中具有抗增殖活性,并被用于各种癌症的研究,如结肠癌。 | |||
T10522 |
BET-IN-6
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Epigenetic Reader Domain | Chromatin/Epigenetic |
BET-IN-6 是一种有效且高亲和力的BRD2/BRD4抑制剂。BET-IN-6 是靶蛋白 BRD2/4 的配体,可用于合成 PROTAC BRD2/BRD4 degrader-1 。 | |||
T72636 | BRD4 Inhibitor-26 | ||
BRD4Inhibitor-26 是一种溴结构域蛋白 4(BRD4)抑制剂/一氧化氮供体。BRD4Inhibitor-26 抑制BRD4(BD1) 和BRD4(BD2),IC50值分别为 0.82 μM 和 1.94 μM。BRD4Inhibitor-26 可用于卵巢癌的研究。 | |||
T78647 |
PROTAC BRD4 Degrader-16
|
PROTACs | PROTAC |
PROTACBRD4Degrader-16是一种高效的PROTAC BRD4降解剂,具有对BRD4(BD1)和BRD4(BD2)分别为34.58 nM及40.23 nM的IC50值。该化合物有效抑制G2/M阶段细胞周期蛋白B1(Cyclin B1)的表达,并显著诱导MV-4-11细胞的细胞凋亡(apoptosis)。 | |||
T63991 | BRD4/CK2-IN-1 | ||
BRD4/CK2-IN-1 是高效的、口服具有活力的 BRD4/CK2 (含溴结构域蛋白 4/酪蛋白激酶 2) 双靶点抑制剂,能够作用于 BRD4 (IC50: 180 nM) 和 CK2 (IC50: 230 nM)。在三阴性乳腺癌 (TNBC) 中,BRD4/CK2-IN-1 能够诱导细胞凋亡和自噬相关的细胞死亡。BRD4/CK2-IN-1 表现出显著的抗癌效果,且没有明显毒性。 | |||
T36628 |
PROTAC BRD4 Degrader-8
PROTAC BRD4 Degrader-8 |
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PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degra... | |||
T74270 |
PROTAC BRD4 Degrader-17
|
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PROTACBRD4 Degrader-17 (compound 13i),作为一种高效的 PROTACBRD4 降解剂,其 IC50 值分别为 29.54 nM(针对 BRD4(BD1))和 3.82 nM(针对 BRD4(BD2))。该化合物有效抑制 G2/M 相的细胞周期蛋白 B1 (Cyclin B1) 的表达,并在 MV-4-11 细胞中显著诱导细胞凋亡(apoptosis)。 | |||
T15399 | GNE-207 | Epigenetic Reader Domain | Chromatin/Epigenetic |
GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells). | |||
T36103 |
TW9
TW9 |
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TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistica... | |||
T36800 |
EN219
|
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EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP hum... | |||
T38381 |
CAY17c
|
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CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,... |