JAK/HDAC-IN-1 是一种有效的 JAK2/HDAC 双重抑制剂，在一些血液学细胞系中具有抗增殖和促凋亡作用。JAK/HDAC-IN-1 对 JAK2 和 HDAC 的 IC50 值分别为 4 和 2 nM。
货号:ajcx38636
CAS:2284621-75-4
分子式:C19H21Cl2N7O2
分子量：450.32
溶解度:DMSO : 20.83 mg/mL (46.26 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively[1].

JAK/HDAC-IN-1 (Compound 8m) exhibits IC50s of 4.8, 7.4 and 49 nM for JAK1, JAK3 and TYK2, and 14, 120, 2470 nM for HDAC2, HDAC6 and HDAC8, respectively[1].

[1]. Liang X, et al. Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies. J Med Chem. 2019 Apr 25;62(8):3898-3923.

Protocol:

JAK2 4nM(IC50)

JAK1 4.8nM(IC50)

JAK3 7.4nM(IC50)

Tyk2 49nM(IC50)

HDAC 2nM(IC50)

HDAC2 14nM(IC50)

HDAC6 120nM(IC50)

HDAC8 2470nM(IC50)