Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11542 |
HDAC-IN-4
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-4 is a selective HDAC6 and HDAC10 inhibitor (pIC50s: 7.2 and 6.8 in BRET assay) with antitumoral activity. | |||
T64261 | HDAC/HSP90-IN-4 | ||
HDAC/HSP90-IN-4 能够明显抑制 HDAC 和 HSP90 的活性,化合物20(HDACIC50= 194 nM; HSP90αIC50= 153 nM)和化合物26((HDACIC50= 360 nM; HSP90αIC50= 77 nM) 具有较强的 HDAC 和 HSP90α抑制效果。这两种化合物都能诱导 HSP90表达并下调 HSP90客户蛋白,而 HSP90客户蛋白在调节癌细胞的生存和侵袭中发挥着重要作用。 | |||
T6865 |
Quisinostat dihydrochloride
Quisinostat 2HCl,Quisinostat (JNJ-26481585) 2HCl,JNJ26854165(Quisinostat) 2HCl,JNJ-26481585 2HCl |
Apoptosis; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) 是一种有口服活性,高效的 pan-HDAC 抑制剂,具有广泛的抗肿瘤活性。它对 HDAC1、HDAC2、HDAC4、HDAC10和HDAC11 的IC50值分别为 0.11 nM、0.33 nM、0.64 nM、0.46 nM 和 0.37 nM。 | |||
T61583 | CDK/HDAC-IN-1 | ||
CDK/HDAC-IN-1 exhibits potent inhibitory activity towards CDK2/4/6 and HDAC6, with IC50 values of 60.9 ± 2.9 nM, 276 ± 22.3 nM, 27.2 ± 4.2 nM, and 128.6 ± 0.4 nM, respectively. | |||
T78708 |
JAK/HDAC-IN-2
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK/HDAC-IN-2 是一款高效的 JAK/HDAC 双靶点抑制剂,能在纳摩尔浓度范围内有效抑制 HDAC3/6 与 JAK1/2。此化合物不仅促进细胞凋亡,还能抑制组蛋白去乙酰化和 STAT3 磷酸化,对血液肿瘤和实体肿瘤细胞展现出了显著的抗增殖效果。 | |||
T83947 |
HDAC4 CHDI Degrader 11
|
||
HDAC4 CHDI Degrader 11是一种高效且选择性的HDAC4降解剂(PROTAC),其在Jurkat E6-1细胞和Jurkat细胞中的DC50值分别为4 nM和6 nM。该化合物由类IIa HDAC抑制剂三氟甲基噁二唑通过连接体与Von Hippel-Lindau (VHL) 蛋白的配体连接而成。在亨廷顿病小鼠细胞模型中,HDAC4 CHDI Degrader 11能强效地降解HDAC4(DC50= 1nM)。在神经母细胞瘤细胞系中,可与P-糖蛋白抑制剂Elacridar联用以实现更有效的降解。 | |||
T36102 |
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline
|
||
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline is a building block and synthetic intermediate.1,2,3,4,5It has been used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histone deacetylase (HDAC) inhibitors, and anticancer compounds.1,2,3It is also a synthetic intermediate in the synthesis of EGFR inhibitors, including erlotinib , with antiproliferative activity.4,5 | |||
T36629 | Givinostat | ||
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... | |||
T36103 |
TW9
TW9 |
||
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... |