Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T73179 |
HDAC-IN-50
|
||
HDAC-IN-50是一种口服活性的有效FGFR和HDAC双重抑制剂,其IC50值针对FGFR1、FGFR2、FGFR3、FGFR4、HDAC1、HDAC2、HDAC6、HDAC8分别为0.18、1.2、0.46、1.4、1.3、1.6、2.6、13 nM。该化合物能诱导(Apoptosis)及使细胞周期在G0/G1期停滞,降低pFGFR1、pERK、pSTAT3的表达,展现出抗肿瘤活性。 | |||
T39990 |
HDAC-IN-26
|
||
HDAC-IN-26 is a highly selective class I HDAC inhibitor with an EC 50 value of 4.7 nM. | |||
T61510 | PIM-1/HDAC-IN-1 | ||
PIM-1/HDAC-IN-1 (compound 4d) is a potent inhibitor of PIM-1, with an IC 50 of 343.87 nM. It also exhibits strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC 50 values of 63.65 and 62.39 nM, respectively. Furthermore, PIM-1/HDAC-IN-1 demonstrates apoptosis-inducing potential in MCF-7 cell lines, specifically inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase [1]. | |||
T63399 |
mTOR/HDAC-IN-1
|
||
mTOR/HDAC-IN-1 (Compound 50) 是一个具有选择性的mTOR 和HDAC 双重抑制剂,对mTOR 和HDAC1的IC50分别为0.49和0.91 nM。 mTOR/HDAC-IN-1 可作为抗癌活性分子 (anti-cancer) 进行研究。 | |||
T61451 | NMDAR/HDAC-IN-1 | ||
NMDAR/HDAC-IN-1 (Compound 9d) is a potent dual inhibitor of N-methyl-D-aspartate receptors (NMDARs) and histone deacetylases (HDACs). It exhibits a high affinity (Ki = 0.59 μM) for NMDARs, while demonstrating significant inhibitory effects on various HDAC isoforms, including HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC 50 values of 2.67 μM, 8.00 μM, 2.21 μM, 0.18 μM, and 0.62 μM, respectively. Moreover, NMDAR/HDAC-IN-1 efficiently crosses the blood-brain barrier [1]. | |||
T72839 |
SHP2/HDAC-IN-1
|
||
SHP2/HDAC-IN-1 是一种变构的 SHP2/HDAC 双重抑制剂,IC50值分别为 20.4 nM (SHP2) 和 25.3 nM ( HDAC1)。SHP2/HDAC-IN-1 通过激活 T 细胞、增强抗原呈递功能和促进细胞因子分泌来触发抗肿瘤免疫反应。SHP2/HDAC-IN-1 可用于癌症的免疫治疗研究。 | |||
T21898 |
MI-192
|
||
MI-192 是一种选择性 HDAC2和 HDAC3抑制剂,IC50分别为 30 nM 和 16 nM。MI-192 比其他 HDAC 异构体对 HDAC2/3 具有更高选择性。MI-192 诱导髓系白血病细胞凋亡 (apoptosis)。抗癌和神经保护活性。 | |||
T61209 | HDAC-IN-27 | ||
HDAC-IN-27 是一种有效的口服活性HDACI 类选择性抑制剂,对 HDAC1-3 的 IC50值范围为 0.43 至 3.01 nM。抗急性髓系白血病 (AML) 活性。 | |||
T9644 |
Triciferol
|
||
Triciferol 作为具有结合了 VDR 激动剂和 HDAC 拮抗剂活性的多重配体发挥作用。Triciferol 直接与 VDR 结合 (IC50=87 nM),在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化,并增强组蛋白乙酰化。Triciferol 在体外癌细胞模型中也表现出有效的抗增殖和细胞毒性活性。 | |||
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... |