BX795

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WARNING: This product is for research use only, not for human or veterinary use.

Description:BX795 is a potent PDK1 inhibitor. BX795 also suppresses MARK1, MARK2, MARK4, NUAK1,

Price and Availability

BX-795, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 401158Name: BX795CAS#: 702675-74-9Chemical Formula: C23H26IN7O2SExact Mass: 591.09134Molecular Weight: 591.47Elemental Analysis:C, 46.71; H, 4.43; I, 21.46; N, 16.58; O, 5.41; S, 5.42

Synonym:BX-795; BX 795; BX795.

IUPAC/Chemical Name:N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide

InChi Key:VAVXGGRQQJZYBL-UHFFFAOYSA-N

InChi Code:InChI=1S/C23H26IN7O2S/c24-18-15-27-22(30-20(18)25-9-5-10-26-21(32)19-8-4-13-34-19)28-16-6-3-7-17(14-16)29-23(33)31-11-1-2-12-31/h3-4,6-8,13-15H,1-2,5,9-12H2,(H,26,32)(H,29,33)(H2,25,27,28,30)

SMILES Code:O=C(N1CCCC1)NC2=CC=CC(NC3=NC=C(I)C(NCCCNC(C4=CC=CS4)=O)=N3)=C2

Technical Data

Additional Information

References

1: Miyabe H, Hyodo M, Nakamura T, Sato Y, Hayakawa Y,Harashima H. A new adjuvant delivery system "cyclic di-GMP/YSK05liposome" for cancer immunotherapy. J Control Release. 2014 Jun28;184:20-7. doi: 10.1016/j.jconrel.2014.04.004. Epub 2014 Apr 13.PubMed PMID: 24727060.

2: Dangelmaier C, Manne BK, Liverani E, Jin J, Bray P, Kunapuli SP. PDK1selectively phosphorylates Thr(308) on Akt and contributes to humanplatelet functional responses. Thromb Haemost. 2014 Mar 3;111(3):508-17.doi: 10.1160/TH13-06-0484. Epub 2013 Dec 19. PubMed PMID: 24352480;PubMed Central PMCID: PMC4079046.

3: Parsons KS, Hsu AC, Wark PA. TLR3 and MDA5 signalling, although notexpression, is impaired in asthmatic epithelial cells in response torhinovirus infection. Clin Exp Allergy. 2014 Jan;44(1):91-101. doi:10.1111/cea.12218. PubMed PMID: 24131248.

4: Sun Q, Sammut B, Wang FM, Kurihara N, Windle JJ, Roodman GD, GalsonDL. TBK1 mediates critical effects of measles virus nucleocapsid protein(MVNP) on pagetic osteoclast formation. J Bone Miner Res. 2014Jan;29(1):90-102. doi: 10.1002/jbmr.2026. PubMed PMID: 23794264; PubMedCentral PMCID: PMC3870038.

5: Minegishi Y, Iejima D, Kobayashi H, Chi ZL, Kawase K, Yamamoto T,Seki T, Yuasa S, Fukuda K, Iwata T. Enhanced optineurin E50K-TBK1interaction evokes protein insolubility and initiates familial primaryopen-angle glaucoma. Hum Mol Genet. 2013 Sep 1;22(17):3559-67. doi:10.1093/hmg/ddt210. Epub 2013 May 12. PubMed PMID: 23669351.

6: Awe JP, Crespo AV, Li Y, Kiledjian M, Byrne JA. BAY11 enhances OCT4synthetic mRNA expression in adult human skin cells. Stem Cell Res Ther.2013 Feb 6;4(1):15. doi: 10.1186/scrt163. PubMed PMID: 23388106; PubMedCentral PMCID: PMC3706837.

7: McIver EG, Bryans J, Birchall K, Chugh J, Drake T, Lewis SJ, OsborneJ, Smiljanic-Hurley E, Tsang W, Kamal A, Levy A, Newman M, Taylor D,Arthur JS, Clark K, Cohen P. Synthesis and structure-activityrelationships of a novel series of pyrimidines as potent inhibitors ofTBK1/IKKε kinases. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7169-73. doi:10.1016/j.bmcl.2012.09.063. Epub 2012 Sep 28. PubMed PMID: 23099093.

8: Sutlu T, Nyström S, Gilljam M, Stellan B, Applequist SE, Alici E.Inhibition of intracellular antiviral defense mechanisms augmentslentiviral transduction of human natural killer cells: implications forgene therapy. Hum Gene Ther. 2012 Oct;23(10):1090-100. doi:10.1089/hum.2012.080. Epub 2012 Sep 10. PubMed PMID: 22779406; PubMedCentral PMCID: PMC3472531.

9: Clark K, Plater L, Peggie M, Cohen P. Use of the pharmacologicalinhibitor BX795 to study the regulation and physiological roles of TBK1and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172phosphorylation and activation. J Biol Chem. 2009 May22;284(21):14136-46. doi: 10.1074/jbc.M109.000414. Epub 2009 Mar 22.PubMed PMID: 19307177; PubMed Central PMCID: PMC2682862.