Key Specifications Table
|Empirical Formula||CAS #|
Pricing & Availability
An invalid quantity was specified. The product quantity has been adjusted.
|5.30758.0001||Glass bottle||5 mg||
|Overview||A cell-permeable tricyclic quinoline-acrylamide analog of BMX-IN-1 (Cat. No. 505021) that covalently modifies Cys481 in the kinase hinge region of Bruton's tyrosine kinase (BTK) and acts as a highly potent, selective, irreversible, and time-dependent inhibitor (IC50 = 6.6 nM). Also, inhibits the activity of bone marrow kinase on chromosome X (BMX) with equal potency (IC50 = 6.7 nM). Shown to be about 300-fold less potent against Cys496Ser mutated BTK. Displays excellent selectivity against a panel of 456 protein kinases, including JAK3, BLK, TEC, ITK, and EGFR and does not affect PI 3-K/mTOR and Raf/MEK/ERK signaling pathways. Diminishes autophosphorylation of BTK on Tyr223 in cells (EC50 = 475 nM) and promotes proteasome-mediated degradation of BTK (EC50 ~ 1 µM in HEK293T cells). Shown to induce cell cycle arrest at G1 phase and induce apoptotic cell death in Ramos cells. Also blocks the proliferation of several B-cell lymphoma cell lines (GI50 = 370, 200, 260,120, and 120 nM for Ramos, U2932, MM1S, RPMI8226, and BCWM.1, respectively).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
|Synonyms||1-(1-Acryloylindolin-6-yl)-9-(1-methyl-1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-2(1H)-one, BMX Inhibitor II, TEC Inhibitor II, Brutonʹs Tyrosine Kinase Inhibitor V, PI 3-K Inhibitor XXI, BTK Inhibitor V, BLK Inhibitor II|
|References||Wu, H., et al. 2014. ACS Chem. Biol. 9, 1068.|
|Primary Target||BMX & BTK|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Wu, H., et al. 2014. ACS Chem. Biol. 9, 1068.|
|White Paper: Further considerations of antibody validation and usage. (EMD)|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.