PAC-1

• CAT Number: I003120
• CAS Number: 315183-21-2
• Molecular Formula: C23H28N4O2
• Molecular Weight: 392.5
• Purity: ≥95%
• Target: Caspase
• Solubility: DMSO 78 mg/ml; Water <1 mg/ml
• Storage: 3 years -20C powder
• IC50: 0.22 uM (EC50) [1]
• InChIKey: YQNRVGJCPCNMKT-LFVJCYFKSA-N

PAC-1(CAT: I003120), also known as Procaspase-Activating Compound 1, is a small molecule that promotes caspase activation and induces apoptosis. It functions by targeting procaspase-3, a precursor form of caspase-3, and facilitating its activation into the active caspase-3 enzyme. PAC-1 has shown potential as an anticancer agent and has been investigated for its therapeutic effects in various cancer types, including glioblastoma, melanoma, and pancreatic cancer. It has also demonstrated synergistic effects when used in combination with other chemotherapeutic agents. PAC-1 represents a promising strategy to promote apoptosis in cancer cells and has garnered interest in cancer research and drug development.

Reference

1:SM-1, a novel PAC-1 derivative, activates procaspase-3 and causes cancer cell apoptosis. Chen Y, Sun M, Ding J, Zhu Q.Cancer Chemother Pharmacol. 2016 Sep;78(3):643-54. doi: 10.1007/s00280-016-3115-6. Epub 2016 Aug 3. PMID: 27488460 2:Molecular evidence of Zn chelation of the procaspase activating compound B-PAC-1 in B cell lymphoma. Sarkar A, Balakrishnan K, Chen J, Patel V, Neelapu SS, McMurray JS, Gandhi V.Oncotarget. 2016 Jan 19;7(3):3461-76. doi: 10.18632/oncotarget.6505. PMID: 26658105 Free PMC Article3:Derivatives of Procaspase-Activating Compound 1 (PAC-1) and their Anticancer Activities. Roth HS, Hergenrother PJ.Curr Med Chem. 2016;23(3):201-41. PMID: 26630918 Free PMC Article4:Synergistic antitumor activity of pro-apoptotic agent PAC-1 with cisplatinum by the activation of CASP3 in pulmonary adenocarcinoma cell line H1299. Huang JQ, Liang HL, Zhang XC, Xie Z, Jin TE.Asia Pac J Clin Oncol. 2016 Mar;12(1):41-51. doi: 10.1111/ajco.12419. Epub 2015 Dec 1. PMID: 26620316 5:Preclinical combination of TP-0903, an AXL inhibitor and B-PAC-1, a procaspase-activating compound with ibrutinib in chronic lymphocytic leukemia. Patel V, Keating MJ, Wierda WG, Gandhi V.Leuk Lymphoma. 2016;57(6):1494-7. doi: 10.3109/10428194.2015.1102243. Epub 2015 Nov 16. No abstract available. PMID: 26440741 6:Targeting executioner procaspase-3 with the procaspase-activating compound B-PAC-1 induces apoptosis in multiple myeloma cells. Zaman S, Wang R, Gandhi V.Exp Hematol. 2015 Nov;43(11):951-962.e3. doi: 10.1016/j.exphem.2015.07.005. Epub 2015 Aug 6. PMID: 26257207 Free PMC Article7:Removal of Metabolic Liabilities Enables Development of Derivatives of Procaspase-Activating Compound 1 (PAC-1) with Improved Pharmacokinetics. Roth HS, Botham RC, Schmid SC, Fan TM, Dirikolu L, Hergenrother PJ.J Med Chem. 2015 May 14;58(9):4046-65. doi: 10.1021/acs.jmedchem.5b00413. Epub 2015 Apr 20. PMID: 25856364 Free PMC Article8:Targeting procaspase-3 with WF-208, a novel PAC-1 derivative, causes selective cancer cell apoptosis. Wang F, Liu Y, Wang L, Yang J, Zhao Y, Wang N, Cao Q, Gong P, Wu C.J Cell Mol Med. 2015 Aug;19(8):1916-28. doi: 10.1111/jcmm.12566. Epub 2015 Mar 8. PMID: 25754465 Free PMC Article9:PAC-1 and isatin derivatives are weak matrix metalloproteinase inhibitors. Sjøli S, Solli AI, Akselsen O, Jiang Y, Berg E, Hansen TV, Sylte I, Winberg JO.Biochim Biophys Acta. 2014 Oct;1840(10):3162-9. doi: 10.1016/j.bbagen.2014.07.011. Epub 2014 Jul 18. PMID: 25046380 10:[Changes and significance of P-selectin and PAC-1 in coronary heart disease before and after stenting]. Hou M, Yu J, Zhang L, Liu C.Zhonghua Yi Xue Za Zhi. 2014 Mar 18;94(10):766-8. Chinese. PMID: 24844962