Kenpaullone

Kenpaullone is a potent inhibitor of CDK1/cyclin B (IC50 = 400 nM), CDK2/cyclin A (IC50 = 680 nM), CDK2/cyclin E (IC50 = 7.5 uM) and CDK5/p25 (IC50 = 850 nM). Kenpaullone inhibits CDK2/cyclin A, CDK2/cyclin E and CDK5/cyclin/p35 (IC50 values are 0.68, 7.5 and 0.85 μM respectively).

Product information

CAS Number: 142273-20-9

Molecular Weight: 327.18

Formula: C16H11BrN2O

Synonym:

NSC-664704

Bromopaullone

azakenpaullone

NSC664704

NSC 664704

Kenpaullone

Chemical Name:    9-bromo-7,12-dihydrobenzo[2,3]azepino[4,5-b]indol-6(5H)-one

Smiles: O=C1CC2=C(NC3=CC=C(Br)C=C32)C2=CC=CC=C2N1

InChiKey: QQUXFYAWXPMDOE-UHFFFAOYSA-N

InChi: InChI=1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Kenpaullone shows much less effect on c-src (IC50, 15 μM), casein kinase 2 (IC50, 20 μM), erk 1 (IC50, 20 μM), and erk 2 (IC50, 9 μM). Kenpaullone acts by competitive inhibition of ATP binding, and the apparent Ki is 2.5 μM. Kenpaullone can inhibit the growth of tumor cells in culture (mean GI50, 43 μM) and causes altered cell cycle progression most clearly revealed under conditions of recovery from serum starvation. Kenpaullone demonstrates a wide range of biological utility, extending from maintenance of pancreatic β cell survival and proliferation to the induction of apoptosis in cancer cells.

References:

1. Gu H, Ding L, Xiong SD, Gao XM, Zheng B. Inhibition of CDK2 promotes inducible regulatory T-cell differentiation through TGFβ-Smad3 signaling pathway. Cell Immunol. 2014 Jul;290(1):138-44. doi: 10.1016/j.cellimm.2014.05.004. Epub 2014 May 27. PubMed PMID: 24978614.
2. Zhang Y, Welzig CM, Picard KL, Du C, Wang B, Pan JQ, Kyriakis JM, Aronovitz MJ, Claycomb WC, Blanton RM, Park HJ, Galper JB. Glycogen synthase kinase-3β inhibition ameliorates cardiac parasympathetic dysfunction in type 1 diabetic Akita mice. Diabetes. 2014 Jun;63(6):2097-113. doi: 10.2337/db12-1459. Epub 2014 Jan 23. PubMed PMID: 24458356; PubMed Central PMCID: PMC4030105.
3. Yoshida H, Kotani H, Kondo T, Tani I, Wei X, Tsuruta S, Kimura A, Asakawa M, Ito M, Nagai S, Yoshimura A. CDK inhibitors suppress Th17 and promote iTreg differentiation, and ameliorate experimental autoimmune encephalomyelitis in mice. Biochem Biophys Res Commun. 2013 Jun 7;435(3):378-84. doi: 10.1016/j.bbrc.2013.04.096. Epub 2013 May 9. PubMed PMID: 23665028.

Products are for research use only. Not for human use.