BX-795

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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2. 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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6. 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.