Kenpaullone


Catalog No. size PriceQuantity
M6457-2 2mg solid $125
M6457-10 10mg solid $522

Description

Cas:142273-20-9

Product Information

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).

 

Chemical Formula: C16H11BrN2O

 

Exact Mass: 326.00548

 

Molecular Weight: 327.18

 

Elemental Analysis: C, 58.74; H, 3.39; Br, 24.42; N, 8.56; O, 4.89

 

Synonym: 

 

NSC664704

NSC-664704

NSC 664704

  • Bromopaullone

  • azakenpaullone

Kenpaullone

 

Chemical Name:  

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

 

InChi Key:

QQUXFYAWXPMDOE-UHFFFAOYSA-N

 

InChi Code:   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)

 

Smiles Code:

O=C(NC1=CC=CC=C12)CC3=C2NC4=C3C=C(Br)C=C4

 

 

Technical Data:

 

Appearance: White to off-white solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

  1. 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.

 

  1. Taei A, Hassani SN, Eftekhari-Yazdi P, Rezazadeh Valojerdi M, Nokhbatolfoghahai M, Masoudi NS, Pakzad M, Gourabi H, Baharvand H. Enhanced generation of human embryonic stem cells from single blastomeres of fair and poor-quality cleavage embryos via inhibition of glycogen synthase kinase β and Rho-associated kinase signaling. Hum Reprod. 2013 Oct;28(10):2661-71. doi: 10.1093/humrep/det309. Epub 2013 Aug 6. PubMed PMID: 23925393.

 

  1. Bahammam M, Black SA Jr, Sume SS, Assaggaf MA, Faibish M, Trackman PC. Requirement for active glycogen synthase kinase-3β in TGF-β1 upregulation of connective tissue growth factor (CCN2/CTGF) levels in human gingival fibroblasts. Am J Physiol Cell Physiol. 2013 Sep 15;305(6):C581-90. doi: 10.1152/ajpcell.00032.2013. Epub 2013 Jul 3. PubMed PMID: 23824844; PubMed Central PMCID: PMC3761177.

 

  1. 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.

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