K252cA PKC inhibitor with selective for PKCA

K252c (CAS 85753-43-1)

K252c | CAS 85753-43-1 is rated 5.0 out of 5 by 1.
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Synonym: Staurosporine Aglycone
Application: A PKC inhibitor with selective for PKCA
CAS Number: 85753-43-1
Purity: 95%
Molecular Weight: 311.4
Molecular Formula: C20H13N3O
* Refer to Certificate of Analysis for lot specific data (including water content).
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K252c is an aglycone, indolocarbazole alkaloid which is a protein kinase inhibitor of the Staurosporine family. K252c is a cell-permeable inhibitor of PKC (protein kinase C) (IC50 = 2.45 μM) that displays approximately 10-fold selectivity over PKA (protein kinase A) (IC50 = 25.7 μM). K252c is cytotoxic for A549 and P388 cells (IC50 = 2-3 mM). K252c also inhibits LACTB (β-lactamase), malate dehydrogenase (MDH2, MDHC, MDH1B) and chymotrypsin (IC50 values are 8, 8 and 10 μM respectively). K252c displays antiviral activity against GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV) (IC50 values range from 0.13-0.32 μM).


References

1. Nakanishi, S., et al. 1986. J. Antibiot. 39: 1066-1071. PMID: 3759658
2. Yasuzawa, T., et al. 1986. J. Antibiot. 39: 1072-1078. PMID: 3759659
3. Rυegg, U.T., et al. 1989. Trends Pharmacol. Sci. 10: 218-220. PMID: 2672462
4. Zimmermann, A., et al. 2000. Antiviral Res. 48: 49-60. PMID: 11080540
5. Prudhomme, M. 2004. Curr Med Chem Anticancer Agents. 4: 509-521. PMID: 15579016
6. Howard-Jones, A.R., et al. 2006. J. Am. Chem. Soc. 128: 12289-12298. PMID: 16967980
7. Hudkins, R.L., et al. 2007. J. Med. Chem. 50: 433-441. PMID: 17266195

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mM), and methanol. Insoluble in water.
Storage :
Store at -20° C
Melting Point :
251.24° C (Predicted)
Boiling Point :
~779.0° C at 760 mmHg (Predicted)
Density :
1.53 g/cm3 (Predicted)
Refractive Index :
n20D 1.94 (Predicted)
IC50 :
protein kinase C: IC50 = 214 nM; protein kinase A: IC50 = 25.7 µM; β-lactamase: IC50 = 8 µM; malate dehydrogenase : IC50 = 8 µM; chymotrypsin: IC50 = 10 µM; GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV) : IC50 = 0.13-0.32 µM (human); calcium/calmodulin-activated phosphodiesterase: IC50 = 297 µM; P388: IC50 = 3.2 µM; lung cancer A549 cells: IC50 = 2 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
3815
MDL Number :
MFCD00236435
SMILES :
C1C2=C3C4=CC=CC=C4NC3=C5C(=C2C(=O)N1)C6=CC=CC=C6N5

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K252c  Product Citations

See how others have used K252c. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 28433711  Chen, YH. et al. 2017. Biochim. Biophys. Acta. 1863: 1492-1499.

PMID: # 21290541  Groom, K. et al. 2011. Chembiochem. 12: 396-400.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Zimmermann et al Zimmermann et al. (PubMed ID 11080540) found that K252c inhibited GCV-sensitive and resistant human cytomegalovirus strains by blocking protein kinase pUL97 function. -SCBT Publication Review
Date published: 2015-07-04
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