PAC1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PAC-1 是一种有效的 procaspase-3 激活剂，EC50 为 0.22 μM，是已知的第一个直接将 procaspase-3 激活为 caspase-3 的小分子。

PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.(In Vitro):PAC-1 activates procaspase-3 with an EC50 of 2.08 μM. PAC-1 exhibits an enhanced zinc chelating ability (EC50= 7.08 μM). PAC-1 induces leukemia cell death with IC50 of 4.03 μM, which is consistent with the values reported by other investigators. PAC-1 treatment also results in death of other malignant cells in a concentration-dependent manner with IC50s ranging from 4.03 to 53.44μM. The overall mean IC50 in the fifteen malignant cell lines is 0.88 mM for WF-210 and 19.40 μM for PAC-1. In contrast, the sensitivity of the normal human cells (PBL, L-02, HUVEC and MCF 10A) to WF-210 is 2.6-fold lower (mean IC50=412.34 μM) than PAC-1 (mean IC50=158.29 μM). Procaspase-activating compound-1 (PAC-1) is the first direct caspase-activating compound discovered. PAC-1 treatment upregulates Ero1α in multiple cell lines, whereas silencing of Ero1α significantly inhibits calcium release from ER and cell death. (In Vivo):To evaluate the in vivo effect of WF-210 on the growth of malignant tumors, we examined the ability of WF-210 to suppress tumor growth in mouse Hep3B and MDA-MB-435 xenograft models. These two cell lines express procaspase-3 at relatively high levels. Tumors induced by xenografts of the liver cancer cell Hep3B are allowed to develop and grow to a size of 100 mm3, after which WF-210 (2.5 mg/kg) or PAC-1 (5.0 mg/kg) is given daily for two weeks by intravenous (i.v.) administration. As shown in both PAC-1 and WF-210 significantly inhibits the growth of Hep3B tumor xenografts.

——

——

Procaspase-activating Compound 1

Apoptosis

Caspase

Procaspase-3

Cancer

——

315183-21-2

392.49

C23H28N4O2

>98% (HPLC)

Ethanol: 16 mg/mL (40.76 mM); DMSO: 78 mg/mL (198.73 mM)

O=C(N/N=C/C1=CC=CC(CC=C)=C1O)CN2CCN(CC3=CC=CC=C3)CC2

(E)-N'-(3-allyl-2-hydroxybenzylidene)-2-(4-benzylpiperazin-1-yl)acetohydrazide

(-20℃)

With Ice Pack

≥ 2 years