BX-795

SKU: orb1307362

Description

BX795

Research Area

Molecular Biology

Key Properties

• CAS Number: 702675-74-9
• MW: 591.5
• Purity: >97%
• Formula: C₂₃H₂₆IN₇O₂S
• SMILES: Ic1cnc(Nc2cccc(NC(=O)N3CCCC3)c2)nc1NCCCNC(=O)c1cccs1
• Target: Kinase
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  IKKε:41 nM|PDK1:6 nM|TBK1:6 nM
• In Vivo:
  BX795 (1 μM) does not inhibit the following tyrosine protein kinases: hepatocyte receptor A2 and B3, Bruton's tyrosine kinase, Syk, and FGFR1. However, its inhibitory effect on the endothelial growth factor receptor is lower than on TBK1. BX795's ability to inhibit the phosphorylation of IRF3 at Ser396 (catalyzed by TBK1) decreases with increasing ATP concentration, indicating its role as an ATP-competitive inhibitor. Additionally, BX795 inhibits NUAK1, MARK1/2/4, VEGFR, and MLK1/2/3 with IC50s of 5, 55, 53, 19, 157, 50, 46, and 42 nM respectively. It also suppresses IRF3-dependent gene transcription and interferon β secretion in macrophages. BX795 blocks IRF3 activation regulated by IKKε and TBK1, reducing IFN-β production and does not activate p38α MAPK and JNK1/2 following TBK1/IKKε inhibition. It impedes IRF3 accumulation in the nucleus post-poly (I:C) treatment and does not affect LPS-induced phosphorylation at Thr229 on p70 ribosomal S6 kinase 1—a target of PDK1—nor does it affect NFκB-dependent gene transcription activation (stimulated by IKKα/β complex, LPS, poly (I:C), IL-1α, or TNFα). BX795 is effective in MEFs stimulated by IL-1α or TNFα, blocking the phosphorylation of p38α MAPK and JNK1/2.
• Cell Research:
  Cells seeded at a low density (1,500–3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average ± S.E. of two or more replicates.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK2/CyclinE, c-Kit, cKit, Chk1, Autophagy, BX 795, BX795, BX-795, IkB, IkB/IKK, IKK, I kappa B kinase, inhibit, IκB, IκB kinase, Inhibitor, PDK-1, PDK1

Compound Identifiers

PubChem CID

10077147