PAC 1A procaspase-activating compound

PAC 1 (CAS 315183-21-2)

PAC 1 | CAS 315183-21-2 is rated 5.0 out of 5 by 1.
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Application: A procaspase-activating compound
CAS Number: 315183-21-2
Purity: >98%
Molecular Weight: 392.5
Molecular Formula: C23H28N4O2
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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PAC 1 is a procaspase-activating compound, which in turn produces caspase-3 (EC50 = 0.22 μM). PAC 1 also activates procaspase-7 in a less efficient manner (EC50 = 4.5 μM). This compound is a proapoptotic, inducing apoptosis in both cancerous and non-cancerous cell lines. The induction of apoptosis is dependent on the concentration of procaspase-3 (IC50 values anre 0.003-1.41 and 5.02=9.98 μM, respectively).


References

Putt et al (2006) Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat.Chem.Biol. 2 543.

Physical State :
Solid
Solubility :
Soluble in 1eq. HCl (75 nM), DMSO (100 mM), deionized water (≤2 mg/mL), water (0.25 mg/mL) at 25° C, ethanol (~5 mg/mL), DMSO:PBS(PH 7.2)(1:3), DMF (~30 mg/ml), and 1:3 solution of ethanol :PBS(PH 7.2) (~0.25 mg/ml).
Storage :
Store at 4° C
Melting Point :
250.41° C (Mean or Weighted MP)
Boiling Point :
580.94° C (Adapted Stein & Brown method)
IC50 :
: IC50 = 3 nM (cancer cells); Adjacent normal tissue: IC50 = 3.2-8.5 µM (cancer cells); Procaspase-3: EC5050 = 0.22 µM; Procaspase-7: EC5050 = 4.5 µM; : IC50 = 0.003-1.41 µM (Cancerous cells); : IC50 = 5.02-9.98 µM (Non-cancerous cells ); Caspase-3: IC50 = 0.35 µM (human); Mutant procaspase-3 with DAD: EC5050 = 2.77 µM; Mutant procaspase-3 with DDA: EC5050 = 113 µM; Mutant procaspase-3 with ADD : EC5050 = 131 µM
pK Values :
pKa: 8.78, pKb: 6.65
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
6851947
MDL Number :
MFCD03302441
SMILES :
C=CCc1cccc(/C=N/NC(=O)CN2CCN(CC2)Cc2ccccc2)c1O

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PAC 1  Product Citations

See how others have used PAC 1. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 20638399  Aziz, G. et al. 2010. Toxicol Appl Pharmacol. -.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Aziz Aziz, G. et al. (PubMed 20638399) used PAC 1, a procaspase-activating compound, to validate that chicken cerebellar granule neurons function as a suitable model to study the mechanisms of interference with apoptosis of PAC 1 and similar compounds. PAC 1 successfully activated caspase-3-dependent cell death and was inhibited by the specific caspase-3-inhibitor Ac-DEVD-cmk. -SCBT Publication Review
Date published: 2015-04-14
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