PAC-1 (Synonyms: Procaspase activating compound 1)

Name: PAC-1
Brand: MedChemExpress
SKU: HY-13523
Rating: 5.0 (7 reviews)

Cat. No.: HY-13523 Purity: 99.88%: Data Sheet
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PAC-1 is a procaspase-3 activator that induces apoptosis in cancer cells with an EC₅₀ of 2.08 μM.

For research use only. We do not sell to patients.

CAS No. : 315183-21-2

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Based on 7 publication(s) in Google Scholar

Other Forms of PAC-1:

PAC-1-d₈ Get quote

7 Publications Citing Use of MCE PAC-1

•Oncotarget. 2017 Feb 14;8(7):12311-12322. [Abstract]

: PAC-1 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 14;8(7):12311-12322. [Abstract]; NB4 cells are treated with 5 μM Z-10 or 50 μM PAC-1 for the indicated time, and the expression of PML-RARα and cleaved caspase3 is analyzed by western blot.

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Description

PAC-1 is a procaspase-3 activator that induces apoptosis in cancer cells with an EC₅₀ of 2.08 μM.

IC₅₀ & Target^[1]

Procaspase-3

2.08 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.51 3 Compound: PAC-1	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25874341]
A549	IC₅₀	2.51 3 Compound: PAC-1	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25874341]
A549	IC₅₀	2.51 3 Compound: PAC-1	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25874341]
B16-F10	IC₅₀	>100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human B16-F10 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human B16-F10 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
B16-F10	IC₅₀	> 100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human B16-F10 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human B16-F10 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
BT-549	IC₅₀	14.3 3 Compound: 19	Cytotoxicity against Smac mimetic-resistant human BT549 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-resistant human BT549 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
B16-F10	IC₅₀	> 100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human B16-F10 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human B16-F10 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
BT-549	IC₅₀	14.3 3 Compound: 19	Cytotoxicity against Smac mimetic-resistant human BT549 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-resistant human BT549 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
BT-549	IC₅₀	14.3 3 Compound: 19	Cytotoxicity against Smac mimetic-resistant human BT549 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-resistant human BT549 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
Cancer cell lines	IC₅₀	0.003 3 Compound: 1, PAC-1	Cytotoxicity against human colon cancer cells after 24 hrs by MTS/PMS assay Cytotoxicity against human colon cancer cells after 24 hrs by MTS/PMS assay	[PMID: 16936720]
Cancer cell lines	IC₅₀	0.003 3 Compound: 1, PAC-1	Cytotoxicity against human colon cancer cells after 24 hrs by MTS/PMS assay Cytotoxicity against human colon cancer cells after 24 hrs by MTS/PMS assay	[PMID: 16936720]
Colon cell	IC₅₀	5.02 3 Compound: 1, PAC-1	Cytotoxicity against human colon cells after 24 hrs by MTS/PMS assay Cytotoxicity against human colon cells after 24 hrs by MTS/PMS assay	[PMID: 16936720]
Colon cell	IC₅₀	5.02 3 Compound: 1, PAC-1	Cytotoxicity against human colon cells after 24 hrs by MTS/PMS assay Cytotoxicity against human colon cells after 24 hrs by MTS/PMS assay	[PMID: 16936720]
EL4	IC₅₀	6.5 3 Compound: 1, PAC-1	Cytotoxicity against mouse EL4 cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against mouse EL4 cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
Cancer cell lines	IC₅₀	0.003 3 Compound: 1, PAC-1	Cytotoxicity against human colon cancer cells after 24 hrs by MTS/PMS assay Cytotoxicity against human colon cancer cells after 24 hrs by MTS/PMS assay	[PMID: 16936720]
EL4	IC₅₀	6.5 3 Compound: 1, PAC-1	Cytotoxicity against mouse EL4 cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against mouse EL4 cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
Colon cell	IC₅₀	5.02 3 Compound: 1, PAC-1	Cytotoxicity against human colon cells after 24 hrs by MTS/PMS assay Cytotoxicity against human colon cells after 24 hrs by MTS/PMS assay	[PMID: 16936720]
HL-60	IC₅₀	0.92 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human HL60 cell death after 72 hrs by MTS/PMS assay Activation of procaspase-3-mediated human HL60 cell death after 72 hrs by MTS/PMS assay	[PMID: 16936720]
HL-60	IC₅₀	0.92 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human HL60 cell death after 72 hrs by MTS/PMS assay Activation of procaspase-3-mediated human HL60 cell death after 72 hrs by MTS/PMS assay	[PMID: 16936720]
HL-60	IC₅₀	0.92 3 Compound: 38; PAC-1	Antitumor activity against human HL-60 cells assessed as cell growth inhibition Antitumor activity against human HL-60 cells assessed as cell growth inhibition	[PMID: 36858050]
EL4	IC₅₀	6.5 3 Compound: 1, PAC-1	Cytotoxicity against mouse EL4 cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against mouse EL4 cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
Hs-578T	IC₅₀	> 100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human Hs 578T cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human Hs 578T cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
Hs-578T	IC₅₀	>100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human Hs 578T cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human Hs 578T cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
HT-29	IC₅₀	0.83 3 Compound: 8; PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 26897090]
HT-29	IC₅₀	1.36 3 Compound: PAC-1	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25171780]
HT-29	IC₅₀	0.83 3 Compound: 7, PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23838381]
HT-29	IC₅₀	0.83 3 Compound: 7, PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23838381]
HT-29	IC₅₀	0.97 3 Compound: 5, PAC-1	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
HT-29	IC₅₀	0.83 3 Compound: 8; PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 26897090]
HT-29	IC₅₀	1.02 3 Compound: PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25874341]
HT-29	IC₅₀	1.02 3 Compound: PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25874341]
HT-29	IC₅₀	1.36 3 Compound: PAC-1	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25171780]
HT-29	IC₅₀	0.97 3 Compound: 5, PAC-1	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
Jurkat	IC₅₀	4.4 3 Compound: 1, PAC-1	Cytotoxicity against human Jurkat cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against human Jurkat cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
Jurkat	IC₅₀	4.4 3 Compound: 1, PAC-1	Cytotoxicity against human Jurkat cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against human Jurkat cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
MCF-10A	IC₅₀	3.2 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human MCF-10A cell death after 72 hrs by MTS/PMS assay Activation of procaspase-3-mediated human MCF-10A cell death after 72 hrs by MTS/PMS assay	[PMID: 16936720]
MCF7	IC₅₀	> 40 3 Compound: PAC-1	Antiproliferative activity against human MCF7 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells after 24 hrs by CCK-8 assay	[PMID: 31015910]
MCF-10A	IC₅₀	3.2 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human MCF-10A cell death after 72 hrs by MTS/PMS assay Activation of procaspase-3-mediated human MCF-10A cell death after 72 hrs by MTS/PMS assay	[PMID: 16936720]
MCF7	IC₅₀	>75 3 Compound: 1, PAC-1	Activation of procaspase-3 in human MCF-7 cells assessed as cell death after 72 hrs Activation of procaspase-3 in human MCF-7 cells assessed as cell death after 72 hrs	[PMID: 16936720]
MCF7	IC₅₀	> 75 3 Compound: 1, PAC-1	Activation of procaspase-3 in human MCF-7 cells assessed as cell death after 72 hrs Activation of procaspase-3 in human MCF-7 cells assessed as cell death after 72 hrs	[PMID: 16936720]
MCF7	IC₅₀	>40 3 Compound: PAC-1	Antiproliferative activity against human MCF7 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells after 24 hrs by CCK-8 assay	[PMID: 31015910]
HL-60	IC₅₀	0.92 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human HL60 cell death after 72 hrs by MTS/PMS assay Activation of procaspase-3-mediated human HL60 cell death after 72 hrs by MTS/PMS assay	[PMID: 16936720]
MDA-MB-231	IC₅₀	3.2 3 Compound: PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25874341]
MCF7	IC₅₀	>75 3 Compound: 38; PAC-1	Antitumor activity against human MCF7 cells assessed as cell growth inhibition Antitumor activity against human MCF7 cells assessed as cell growth inhibition	[PMID: 36858050]
HL-60	IC₅₀	0.92 3 Compound: 38; PAC-1	Antitumor activity against human HL-60 cells assessed as cell growth inhibition Antitumor activity against human HL-60 cells assessed as cell growth inhibition	[PMID: 36858050]
MDA-MB-231	IC₅₀	4.6 3 Compound: 8; PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 26897090]
MDA-MB-231	IC₅₀	4.8 3 Compound: PAC-1	Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by MTT assay	[PMID: 25171780]
HT-29	IC₅₀	0.83 3 Compound: 7, PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23838381]
MDA-MB-231	IC₅₀	4.6 3 Compound: 7, PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 23838381]
HT-29	IC₅₀	0.83 3 Compound: 8; PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 26897090]
MDA-MB-231	IC₅₀	3.2 3 Compound: PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25874341]
MDA-MB-231	IC₅₀	4.7 3 Compound: 19	Cytotoxicity against Smac mimetic-sensitive human MDA-MB-231 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-sensitive human MDA-MB-231 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
MDA-MB-231	IC₅₀	4.8 3 Compound: PAC-1	Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by MTT assay	[PMID: 25171780]
MDA-MB-231	IC₅₀	4.6 3 Compound: 7, PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 23838381]
HT-29	IC₅₀	0.97 3 Compound: 5, PAC-1	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
HT-29	IC₅₀	1.02 3 Compound: PAC-1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25874341]
MDA-MB-231	IC₅₀	4.6 3 Compound: 8; PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 26897090]
MDA-MB-231	IC₅₀	6.11 3 Compound: 5, PAC-1	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
HT-29	IC₅₀	1.36 3 Compound: PAC-1	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25171780]
MDA-MB-231	IC₅₀	6.11 3 Compound: 5, PAC-1	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
MDA-MB-453	IC₅₀	2 3 Compound: 19	Cytotoxicity against Smac mimetic-resistant human MDA-MB-453 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-resistant human MDA-MB-453 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
MDA-MB-231	IC₅₀	4.7 3 Compound: 19	Cytotoxicity against Smac mimetic-sensitive human MDA-MB-231 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-sensitive human MDA-MB-231 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
MKN-45	IC₅₀	0.82 3 Compound: 8; PAC-1	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 26897090]
Hs-578T	IC₅₀	> 100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human Hs 578T cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human Hs 578T cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
MDA-MB-453	IC₅₀	2 3 Compound: 19	Cytotoxicity against Smac mimetic-resistant human MDA-MB-453 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-resistant human MDA-MB-453 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
MKN-45	IC₅₀	0.82 3 Compound: 7, PAC-1	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 23838381]
Jurkat	IC₅₀	4.4 3 Compound: 1, PAC-1	Cytotoxicity against human Jurkat cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against human Jurkat cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
MKN-45	IC₅₀	2.61 3 Compound: PAC-1	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 25171780]
MKN-45	IC₅₀	2.61 3 Compound: PAC-1	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 25171780]
MKN-45	IC₅₀	0.82 3 Compound: 7, PAC-1	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 23838381]
KE-37	IC₅₀	241.66 1 Compound: PAC-1	Anticancer activity against human KE-37 cells assessed as reduction in cell viability Anticancer activity against human KE-37 cells assessed as reduction in cell viability	[PMID: 33774345]
NCI-H226	IC₅₀	0.35 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human NCI-H226 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human NCI-H226 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
MCF-10A	IC₅₀	3.2 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human MCF-10A cell death after 72 hrs by MTS/PMS assay Activation of procaspase-3-mediated human MCF-10A cell death after 72 hrs by MTS/PMS assay	[PMID: 16936720]
MKN-45	IC₅₀	0.82 3 Compound: 8; PAC-1	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 26897090]
NCI-H226	IC₅₀	1.02 3 Compound: PAC-1	Antiproliferative activity against human NCI-H226 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H226 cells after 72 hrs by MTT assay	[PMID: 25171780]
MCF7	IC₅₀	> 40 3 Compound: PAC-1	Antiproliferative activity against human MCF7 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells after 24 hrs by CCK-8 assay	[PMID: 31015910]
NCI-H226	IC₅₀	0.35 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human NCI-H226 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human NCI-H226 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
NCI-H460	IC₅₀	1.25 3 Compound: PAC-1	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 25874341]
NCI-H226	IC₅₀	1.02 3 Compound: PAC-1	Antiproliferative activity against human NCI-H226 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H226 cells after 72 hrs by MTT assay	[PMID: 25171780]
NCI-H460	IC₅₀	3.57 3 Compound: 5, PAC-1	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
MCF7	IC₅₀	> 75 3 Compound: 1, PAC-1	Activation of procaspase-3 in human MCF-7 cells assessed as cell death after 72 hrs Activation of procaspase-3 in human MCF-7 cells assessed as cell death after 72 hrs	[PMID: 16936720]
NCI-H226	IC₅₀	0.35 3 Compound: 38; PAC-1	Antitumor activity against human NCI-H226 cells assessed as cell growth inhibition Antitumor activity against human NCI-H226 cells assessed as cell growth inhibition	[PMID: 36858050]
PBL	IC₅₀	123.81 3 Compound: 8; PAC-1	Cytotoxicity against human PBL cells after 72 hrs by MTT assay Cytotoxicity against human PBL cells after 72 hrs by MTT assay	[PMID: 26897090]
MCF7	IC₅₀	> 75 3 Compound: 38; PAC-1	Antitumor activity against human MCF7 cells assessed as cell growth inhibition Antitumor activity against human MCF7 cells assessed as cell growth inhibition	[PMID: 36858050]
PC-12	EC₅₀	122 3 Compound: 2, PAC-1	Induction of apoptosis in rat PC12 cells after 24 hrs by trypan blue exclusion assay Induction of apoptosis in rat PC12 cells after 24 hrs by trypan blue exclusion assay	[PMID: 23859779]
MDA-MB-231	IC₅₀	3.2 3 Compound: PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25874341]
MDA-MB-231	IC₅₀	4.6 3 Compound: 7, PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 23838381]
SK-N-SH	IC₅₀	3.06 3 Compound: PAC-1	Antiproliferative activity against human SK-N-SH cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-SH cells after 72 hrs by MTT assay	[PMID: 25171780]
NCI-H460	IC₅₀	1.25 3 Compound: PAC-1	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 25874341]
MDA-MB-231	IC₅₀	4.6 3 Compound: 8; PAC-1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 26897090]
U-937	IC₅₀	10.2 3 Compound: 1, PAC-1	Cytotoxicity against human U937 cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against human U937 cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
NCI-H460	IC₅₀	3.57 3 Compound: 5, PAC-1	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
MDA-MB-231	IC₅₀	4.7 3 Compound: 19	Cytotoxicity against Smac mimetic-sensitive human MDA-MB-231 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-sensitive human MDA-MB-231 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
U-937	IC₅₀	4.8 3 Compound: 1, PAC-1	Cytotoxicity against human U937 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human U937 cells after 72 hrs by sulforhodamine B assay	[PMID: 19708658]
PBL	IC₅₀	123.81 3 Compound: 8; PAC-1	Cytotoxicity against human PBL cells after 72 hrs by MTT assay Cytotoxicity against human PBL cells after 72 hrs by MTT assay	[PMID: 26897090]
U-937	IC₅₀	6 3 Compound: PAC-1	Antiproliferative activity against human procaspase-3 over-expressing U937 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human procaspase-3 over-expressing U937 cells after 24 hrs by CCK-8 assay	[PMID: 31015910]
MDA-MB-231	IC₅₀	4.8 3 Compound: PAC-1	Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by MTT assay	[PMID: 25171780]
PC-12	EC₅₀	122 3 Compound: 2, PAC-1	Induction of apoptosis in rat PC12 cells after 24 hrs by trypan blue exclusion assay Induction of apoptosis in rat PC12 cells after 24 hrs by trypan blue exclusion assay	[PMID: 23859779]
MDA-MB-231	IC₅₀	6.11 3 Compound: 5, PAC-1	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
UACC-62	IC₅₀	> 100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human UACC62 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human UACC62 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
SK-N-SH	IC₅₀	3.06 3 Compound: PAC-1	Antiproliferative activity against human SK-N-SH cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-SH cells after 72 hrs by MTT assay	[PMID: 25171780]
MDA-MB-453	IC₅₀	2 3 Compound: 19	Cytotoxicity against Smac mimetic-resistant human MDA-MB-453 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay Cytotoxicity against Smac mimetic-resistant human MDA-MB-453 cells assessed as growth inhibition after 24 hrs by CellTiter-Glo assay	[PMID: 27578248]
MKN-45	IC₅₀	0.82 3 Compound: 7, PAC-1	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 23838381]
U-937	IC₅₀	6 3 Compound: PAC-1	Antiproliferative activity against human procaspase-3 over-expressing U937 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human procaspase-3 over-expressing U937 cells after 24 hrs by CCK-8 assay	[PMID: 31015910]
MKN-45	IC₅₀	0.82 3 Compound: 8; PAC-1	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 26897090]
U-937	IC₅₀	4.8 3 Compound: 1, PAC-1	Cytotoxicity against human U937 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human U937 cells after 72 hrs by sulforhodamine B assay	[PMID: 19708658]
MKN-45	IC₅₀	2.61 3 Compound: PAC-1	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 25171780]
U-937	IC₅₀	10.2 3 Compound: 1, PAC-1	Cytotoxicity against human U937 cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against human U937 cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
UACC-62	IC₅₀	>100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human UACC62 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human UACC62 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
NCI-H226	IC₅₀	0.35 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human NCI-H226 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human NCI-H226 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]
NCI-H226	IC₅₀	0.35 3 Compound: 38; PAC-1	Antitumor activity against human NCI-H226 cells assessed as cell growth inhibition Antitumor activity against human NCI-H226 cells assessed as cell growth inhibition	[PMID: 36858050]
NCI-H226	IC₅₀	1.02 3 Compound: PAC-1	Antiproliferative activity against human NCI-H226 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H226 cells after 72 hrs by MTT assay	[PMID: 25171780]
NCI-H446	IC₅₀	2326.69 3 Compound: PAC-1	Anticancer activity against human NCI-H446 cells assessed as reduction in cell viability Anticancer activity against human NCI-H446 cells assessed as reduction in cell viability	[PMID: 33774345]
NCI-H460	IC₅₀	1.25 3 Compound: PAC-1	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 25874341]
NCI-H460	IC₅₀	3.57 3 Compound: 5, PAC-1	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23059545]
PBL	IC₅₀	123.81 3 Compound: 8; PAC-1	Cytotoxicity against human PBL cells after 72 hrs by MTT assay Cytotoxicity against human PBL cells after 72 hrs by MTT assay	[PMID: 26897090]
PC-12	EC₅₀	122 3 Compound: 2, PAC-1	Induction of apoptosis in rat PC12 cells after 24 hrs by trypan blue exclusion assay Induction of apoptosis in rat PC12 cells after 24 hrs by trypan blue exclusion assay	[PMID: 23859779]
SK-N-SH	IC₅₀	3.06 3 Compound: PAC-1	Antiproliferative activity against human SK-N-SH cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-SH cells after 72 hrs by MTT assay	[PMID: 25171780]
U-937	IC₅₀	10.2 3 Compound: 1, PAC-1	Cytotoxicity against human U937 cells assessed as cell death after 72 hrs by sulforhodamine B assay Cytotoxicity against human U937 cells assessed as cell death after 72 hrs by sulforhodamine B assay	[PMID: 25856364]
U-937	IC₅₀	4.8 3 Compound: 1, PAC-1	Cytotoxicity against human U937 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human U937 cells after 72 hrs by sulforhodamine B assay	[PMID: 19708658]
U-937	IC₅₀	6 3 Compound: PAC-1	Antiproliferative activity against human procaspase-3 over-expressing U937 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human procaspase-3 over-expressing U937 cells after 24 hrs by CCK-8 assay	[PMID: 31015910]
UACC-62	IC₅₀	> 100 3 Compound: 1, PAC-1	Activation of procaspase-3-mediated human UACC62 cell death after 24 hrs by MTS/PMS assay Activation of procaspase-3-mediated human UACC62 cell death after 24 hrs by MTS/PMS assay	[PMID: 16936720]

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)^[1]. 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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

392.49

Formula

C₂₃H₂₈N₄O₂

CAS No.

315183-21-2

Appearance

Solid

Color

White to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (127.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5478 mL	12.7392 mL	25.4784 mL
5 mM	0.5096 mL	2.5478 mL	5.0957 mL
10 mM	0.2548 mL	1.2739 mL	2.5478 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (277 KB) SDS (597 KB)

COA (243 KB) HNMR (279 KB) RP-HPLC (257 KB) MS (67 KB)

Handling Instructions (2659 KB)

References

[1]. Wang F, et al. A novel small-molecule activator of procaspase-3 induces apoptosis in cancer cells and reduces tumor growth in human breast, liver and gallbladder cancer xenografts. Mol Oncol. 2014 Dec;8(8):1640-52. [Content Brief]

[2]. Seervi M, et al. ERO1α-dependent endoplasmic reticulum-mitochondrial calcium flux contributes to ER stress and mitochondrial permeabilization by procaspase-activating compound-1 (PAC-1). Cell Death Dis. 2013 Dec 19;4:e968. [Content Brief]

[3]. Putt KS, et al. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50. [Content Brief]

Kinase Assay ^[1]	Various concentrations of WF-210 or PAC-1 are added to procaspase-3 in buffer containing 50 mM HEPES, 0.1% CHAPS, 10% glycerol, 100 mM NaCl, 0.1 mM EDTA, 10 mM DTT pH 7.4,and incubated for 12 h at 37°C. The final volume is 10 mL and the final concentration of procaspase-3 is 1 mM. Then 40 mL of the substrate Ac-DEVD-pNA (final concentration 0.4 mM) in buffer containing 50 mM HEPES pH 7.4, 100 mM NaCl, 10 mM DTT, 0.1 mM EDTA disodium salt, 0.10% CHAPS, 10% glycerol is added and the absorbance of the plate is read at 405 nm for a total of 1 h. The slope of the linear portion for each well is determined as the enzyme activity^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cell viability is measured using the MTT method or the Cell Titer-Glo luminescent assay. For the MTT assay, the cells (1×10⁵ cells/mL) are seeded into 96- well culture plates. After overnight incubation, cells are treated with various concentrations of agents (PAC-1, WF-210 or other agents) for 24 or 72 h. Then 10 mL MTT solution (2.5 mg/mL in PBS) is added to each well, and the plates are incubated for an additional 4 h at 37°C. After centrifugation (2500 rpm, 10min), the medium containing MTT is aspirated, and100mL DMSO is added. The optical density of each well is measured at 570 nm with a Biotek Synergy HT Reader. The Cell Titer-Glo kit is used to determine the relative levels of intracellular ATP as a biomarker for live cells^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] To determine the in vivo anti-tumor activity of WF-210, viable human gallbladder cancer GBC-SD cells (5×10⁶/100 mL PBS per mouse), human breast cancer MDA-MB-435 cells (1×10⁷/100 mL PBS per mouse), human liver cancer Hep3B cells (5×10⁶/100 mL PBS per mouse) and human breast cancer MCF-7 cells (1×10⁷/100 mL PBS per mouse) are subcutaneously (s.c.) injected into the right flank of 7- to 8-week old male SCID mice or Balb/c nude mice. Cell numbers are confirmed by trypan blue staining prior to injection. Specially, MCF-7 xenograft mice are also administered with the hormone 17-beta-estradiol (3 mg/kg) on alternate days. When the average s.c. tumor volume reached 100 mm³, mice are randomly divided into various treatment and control groups (eight mice per group). Tumor size is measured once every two days with a caliper (calculated volume=shortest diameter²×longest diameter/2). Body weight, diet consumption and tumor size are recorded once every two days. After two or four weeks, mice are sacrificed and tumors are excised and stored at -80°C until further analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Wang F, et al. A novel small-molecule activator of procaspase-3 induces apoptosis in cancer cells and reduces tumor growth in human breast, liver and gallbladder cancer xenografts. Mol Oncol. 2014 Dec;8(8):1640-52. [Content Brief] [2]. Seervi M, et al. ERO1α-dependent endoplasmic reticulum-mitochondrial calcium flux contributes to ER stress and mitochondrial permeabilization by procaspase-activating compound-1 (PAC-1). Cell Death Dis. 2013 Dec 19;4:e968. [Content Brief] [3]. Putt KS, et al. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5478 mL	12.7392 mL	25.4784 mL	63.6959 mL
	5 mM	0.5096 mL	2.5478 mL	5.0957 mL	12.7392 mL
	10 mM	0.2548 mL	1.2739 mL	2.5478 mL	6.3696 mL
	15 mM	0.1699 mL	0.8493 mL	1.6986 mL	4.2464 mL
	20 mM	0.1274 mL	0.6370 mL	1.2739 mL	3.1848 mL
	25 mM	0.1019 mL	0.5096 mL	1.0191 mL	2.5478 mL
	30 mM	0.0849 mL	0.4246 mL	0.8493 mL	2.1232 mL
	40 mM	0.0637 mL	0.3185 mL	0.6370 mL	1.5924 mL
	50 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2739 mL
	60 mM	0.0425 mL	0.2123 mL	0.4246 mL	1.0616 mL
	80 mM	0.0318 mL	0.1592 mL	0.3185 mL	0.7962 mL
	100 mM	0.0255 mL	0.1274 mL	0.2548 mL	0.6370 mL

PAC-1 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PAC-1315183-21-2Procaspase activating compound 1PAC1PAC 1Procaspase activating compound1Procaspase activating compound-1CaspaseAutophagyApoptosisInhibitorinhibitorinhibit

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PAC-1 (Synonyms: Procaspase activating compound 1)

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