| Bioactivity | JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers[1]. |
| Invitro | JAK/HDAC-IN-2 (化合物 21) 对 K562、HL-60 和 HEL 细胞表现出很强的抗增殖活性 (IC50 分别为 1.87、2.26 和 0.33 μM)；抑制四种实体瘤细胞 MCF-7、HeLa、A549 和 PC-3 的增殖 (IC50 分别为 1.83、2.88、0.73 和 2.52 μM)[1]。 JAK/HDAC-IN-2 (1, 5 μM; 24 小时) 在 HEL 细胞中具有优异的促凋亡活性，在 A549 细胞中具有中等的促凋亡活性[1]。 JAK/HDAC-IN-2 (1, 5 μM; 24 小时) 通过抑制 HDAC 和 JAK，显着抑制血液恶性肿瘤 HEL 细胞以及实体瘤 A549 细胞中的组蛋白去乙酰化和 STAT3 磷酸化[1] 。 Apoptosis Analysis[1] Cell Line: |
| In Vivo | JAK/HDAC-IN-2 (化合物 21; 50 mg/kg; 腹膜内注射; 每天一次; 连续 18 天) 在体内对血液恶性肿瘤 HEL 和实体瘤 A549 中表现出有效的抗肿瘤活性[1]。 Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1]. |
| Name | JAK/HDAC-IN-2 |
| Formula | C28H38N6O5S |
| Molar Mass | 570.70 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Qianqian Qiu, et al. Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers. J Med Chem. 2023 Apr 27;66(8):5753-5773. |