PAC-1

PAC-1 activates procaspase-3 with an EC50 of 2.08 μM and demonstrates enhanced zinc chelating ability with an EC50 of 7.08 μM. It induces leukemia cell death with an IC50 of 4.03 μM, consistent with values reported by other investigators. Additionally, PAC-1 induces death of other malignant cells in a concentration-dependent manner, with IC50 values ranging from 4.03 to 53.44 μM. The overall mean IC50 in fifteen malignant cell lines is 0.88 mM for WF-210 and 19.40 μM for PAC-1. In contrast, the sensitivity of normal human cells (PBL, L-02, HUVEC, and MCF 10A) to WF-210 is 2.6-fold lower (mean IC50=412.34 μM) than to PAC-1 (mean IC50=158.29 μM)¹. Procaspase-activating PAC-1 is the initial direct caspase-activating compound identified. PAC-1 treatment induces the upregulation of Ero1α in various cell lines, while the suppression of Ero1α notably impedes calcium release from the endoplasmic reticulum (ER) and cell death².

PAC-1 activates procaspase-3 with an EC50 of 2.08 μM and demonstrates enhanced zinc chelating ability with an EC50 of 7.08 μM. It induces leukemia cell death with an IC50 of 4.03 μM, consistent with values reported by other investigators. Additionally, PAC-1 induces death of other malignant cells in a concentration-dependent manner, with IC50 values ranging from 4.03 to 53.44 μM. The overall mean IC50 in fifteen malignant cell lines is 0.88 mM for WF-210 and 19.40 μM for PAC-1. In contrast, the sensitivity of normal human cells (PBL, L-02, HUVEC, and MCF 10A) to WF-210 is 2.6-fold lower (mean IC50=412.34 μM) than to PAC-1 (mean IC50=158.29 μM)¹.

Procaspase-activating PAC-1 is the initial direct caspase-activating compound identified. PAC-1 treatment induces the upregulation of Ero1α in various cell lines, while the suppression of Ero1α notably impedes calcium release from the endoplasmic reticulum (ER) and cell death².

To assess the in vivo impact of WF-210 on malignant tumor growth, we investigated its capacity to impede tumor growth in mouse Hep3B and MDA-MB-435 xenograft models. These cell lines exhibit relatively high levels of procaspase-3 expression. Tumors induced by the xenografts of Hep3B liver cancer cells were allowed to develop and grow to a size of 100 mm^3, following which WF-210 (2.5 mg/kg) or PAC-1 (5.0 mg/kg) was administered intravenously (i.v.) daily for two weeks. As demonstrated, both PAC-1 and WF-210 significantly inhibit the growth of Hep3B tumor xenografts¹.

To assess the in vivo impact of WF-210 on malignant tumor growth, we investigated its capacity to impede tumor growth in mouse Hep3B and MDA-MB-435 xenograft models. These cell lines exhibit relatively high levels of procaspase-3 expression. Tumors induced by the xenografts of Hep3B liver cancer cells were allowed to develop and grow to a size of 100 mm^3, following which WF-210 (2.5 mg/kg) or PAC-1 (5.0 mg/kg) was administered intravenously (i.v.) daily for two weeks. As demonstrated, both PAC-1 and WF-210 significantly inhibit the growth of Hep3B tumor xenografts¹.

溶解方案(细胞实验)

DMSO 中的溶解度 : 50 mg/mL (127.39 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)|H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.5 mg/mL (6.37 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: 2.5 mg/mL (6.37 mM); 悬浊液; 超声助溶 此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案 三": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (6.37 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"