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S6 kinase&PKD-1

BX-795 (702675-74-9)

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

 

Not Intended for Therapeutic Use. For research use only.

CAS: 702675-74-9 Category

BX-795 (702675-74-9) Description:

BX-795 was initially characterized as a potent inhbitor of 3-phosphoinositide-dependent kinase-1. Additional studies with BX-795 have shown that the molecule is also a potent dual inhibitor of IKKe and TBK1 which are known to regulate the expression of interferons via the phosphorylation of interferon regulatory factor 3 (IRF3).

BX-795 competes for the ATP (adenosine triphosphate) binding pocket of 3-phosphoinositide-dependent kinase-1 (PDK1) with its substrate ATP. In vitro assays reveal that BX-795 might inhibit Unc-51 (serine/threonine-protein kinase)-like autophagy activating kinase (ULK1).

BX-795 (702675-74-9) Specifications:

Product Name BX-795
Synonym BX-795; BX 795; BX795.
Chemical Name N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
Drug Class A potent PDK1 inhibitor
Purity ≥98% (HPLC)
CAS Number 702675-74-9
Molecular Formula C23H26IN7O2S
Molecular Weight 591.5
Monoisotopic Mass 591.5 g/mol
MDL number MFCD26406408
InChIKey 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 O=C(N1CCCC1)NC2=CC=CC(NC3=NC=C(I)C(NCCCNC(C4=CC=CS4)=O)=N3)=C2
Form A crystalline solid
Color White to light brown
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application BX-795 hydrochloride has been used to study the effect of kinase inhibition on human endogenous retroviruses (HERVs) transcription activation

 


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RIDADR NONH for all modes of transport

References:

[1]. Miyabe H, Hyodo M, Nakamura T, Sato Y, Hayakawa Y, Harashima H. A new adjuvant delivery system ‘cyclic di-GMP/YSK05 liposome’ for cancer immunotherapy. J Control Release. 2014 Jun 28;184:20-7. doi: 10.1016/j.jconrel.2014.04.004. Epub 2014 Apr 13. PubMed PMID: 24727060.

[2].Parsons KS, Hsu AC, Wark PA. TLR3 and MDA5 signalling, although not expression, is impaired in asthmatic epithelial cells in response to rhinovirus infection. Clin Exp Allergy. 2014 Jan;44(1):91-101. doi: 10.1111/cea.12218. PubMed PMID: 24131248.

[3].Awe JP, Crespo AV, Li Y, Kiledjian M, Byrne JA. BAY11 enhances OCT4 synthetic mRNA expression in adult human skin cells. Stem Cell Res Ther. 2013 Feb 6;4(1):15. doi: 10.1186/scrt163. PubMed PMID: 23388106; PubMed Central PMCID: PMC3706837.

[4].Tamgüney, T., Zhang, C., Fiedler, D., et al. Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells Experimental Cell Research 314(11-12), 2299-2312 (2008).

[5]. Feldman, R.I., Wu, J.M., Polokoff, M.A., et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1 The Journal of Biological Chemisty 280(20), 19867-19874 (2005).