Name: DPP9-IN-2
Brand: TargetMol
SKU: T214331
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

10-14周

50 mg

待询

10-14周

生物活性

产品描述	DPP9-IN-2 is a selective and potent orally active inhibitor of dipeptidyl peptidase 9 (DPP9), with an IC50 value of 12.9 nM. It exhibits a selectivity index of 59 for DPP8 and shows no significant inhibitory activity on related peptidases, including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 can induce pyroptosis in cancer cells and demonstrates modest synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitors. This compound is applicable for research in cancer and infection.
靶点活性	DPP9:12.9 nM
体外活性	DPP9-IN-2 (Compound 6e) (0.05-5 μM; 24-48 h) 在 THP-1 细胞中能够诱导焦亡，促使 LDH 释放并加强 SYTOX Green 的摄取。DPP9-IN-2 (0.5-5 μM; 24 h) 所导致的焦亡依赖于 DPP9、CASP1 和 GSDMD。在 DPP9 敲低、CASP1 敲除或 GSDMD 敲除的 THP-1 细胞中，焦亡作用受到显著抑制或延迟。DPP9-IN-2 (5 μM) 当与非核苷类逆转录酶抑制剂如 Efavirenz 和 Rilpivirine 联合使用时，在 MT-4 细胞中表现出较弱的协同抗 HIV-1 活性。
体内活性	DPP9-IN-2 (Compound 6e) 通过静脉注射 5 mg/kg 或口服 20 mg/kg，在 Wistar 大鼠中促进 CD3⁻CD11b⁻ 白细胞（如 B 细胞和 NK 细胞）的坏死率增加。

化学信息

分子量	541.64
分子式	C₃₃H₃₃F₂N₃O₂
CAS No.	3020859-44-0
Smiles	O=C(NC12CC3CC(C1)CC(NCC(=O)N4CC5=CC=C(F)C=C5C4)(C3)C2)C6=CC=C(C=C6)C=7C=CC(F)=CC7

储存&溶解度

存储	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准

DPP9-IN-2