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BX-795 is a multi-kinase inhibitor that is an ATP-competitive inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1) and TANK-binding kinase 1 (TBK1; IC50s = 6 and 11 nM, respectively).{24213,24248} It also inhibits the CAMK family kinases AMPK-related kinase 5 (NUAK1; IC50 = 5 nM) and microtubule affinity-regulating kinase 1 (MARK1), MARK2, MARK3, and MARK4 (IC50s = 55, 53, 81, and 19 nM, respectively), as well as the MAP3K kinases mixed-lineages kinase 1 (MLK1), MLK2, and MLK3 (IC50s = 50, 46, and 42 nM, respectively). BX-795 is selective for these kinases over five additional kinases (IC50s = >1,100 nM) but does inhibit the receptor tyrosine kinase VEGFR, as well as I?B kinase ? (I???) and Aurora B kinase (IC50s = 41 and 31 nM, respectively).{24213} It inhibits phosphorylation of Akt at Thr308 and p70 ribosomal S6 kinase 1 (p70S6K1) at Thr389 in PC3 prostate cancer cells (IC50 = 300 nM).{24213} BX-795 (1 µM) also inhibits the secretion of IFN-? induced by LPS or poly(I:C) in RAW 264.7 macrophages.{24248} It inhibits the proliferation of PC3 prostate and MDA-MB-468 breast cancer cells (IC50s = 250 and 720 nM, respectively). BX-795 (5 µM) inhibits the proliferation of PDK1-/- murine embryonic stem cells expressing either wild-type PDK1 or PDK1 with an alanine-to-glycine (L159G) mutation.{24247}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 10 mg, 25 mg, 5 mg, 50 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 702675-74-9 |
| Molecular formula | C23H26IN7O2S |
| Smiles | [H]N(CCCN(C(C1=CC=CS1)=O)[H])C2=C(I)C=NC(N([H])C3=CC(N(C(N4CCCC4)=O)[H])=CC=C3)=N2 |
| Molecular weight | 591,5 |
| Custom code | 2930.90 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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