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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T27083 |
Crebinostat
|
Epigenetic Reader Domain; Histone Acetyltransferase; HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂,对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用, IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性,增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化,并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。 | |||
T36103 |
TW9
TW9 |
Others | Others |
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... | |||
T79713 |
JMJD3/HDAC-IN-1
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
JMJD3/HDAC-IN-1 (compound A5b) 是靶向 JMJD3 和 HDAC1(IC50=16 nM)的双重抑制剂。它能够促进 H3K27 高甲基化和 H3K9 高乙酰化,并通过裂解 caspase-7 和 PARP 导致细胞凋亡。此外,JMJD3/HDAC-IN-1 对抑制癌细胞克隆形成、迁移和侵袭也表现出有效性。 | |||
T36629 |
Givinostat
|
Others | Others |
Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1... | |||
T38381 |
CAY17c
|
Others | Others |
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,... |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01471 |
HDAC1 Protein, Human, Recombinant (His & SUMO)
Histone deacetylase 1,Protein |
Human | E. coli |
HDAC1 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 71.1 kDa and the accession number is Q13547. |