Description
BX-795 is a potent PDK1 inhibitor. BX-795 also suppresses MARK1, MARK2, MARK4, NUAK1,
Product information
CAS Number: 702675-74-9
Molecular Weight: 591.47
Formula: C23H26IN7O2S
Synonym:
BX 795
BX795
BX-795
Chemical Name: N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
Smiles: O=C(NC1=CC(=CC=C1)NC1=NC(NCCCNC(=O)C2=CC=CS2)=C(I)C=N1)N1CCCC1
InChiKey: VAVXGGRQQJZYBL-UHFFFAOYSA-N
InChi: 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)
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:
BX-795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX-795 potently inhibits tumor cell growth on plastic with IC50 of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX-795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively. In addition, BX-795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. In platelet physiological responses, BX-795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation.
References:
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- Dangelmaier C, Manne BK, Liverani E, Jin J, Bray P, Kunapuli SP. PDK1 selectively phosphorylates Thr(308) on Akt and contributes to human platelet 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.
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- 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.
Products are for research use only. Not for human use.
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