530758 Sigma-AldrichBMX/BTK Inhibitor II, QL47 - CAS 1469988-75-7 - Calbiochem
A cell-permeable, highly potent, selective, irreversible inhibitor of BTK (IC₅₀ = 6.6 nM).
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Sinónimos: 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
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Tabla espec. clave
| CAS # | Empirical Formula |
|---|---|
| 1469988-75-7 | C₂₇H₂₁N₅O₂ |
Products
| Número de referencia | Embalaje | Cant./Env. | |
|---|---|---|---|
| 5307580001 | Frasco de vidrio | 5 mg |
| Description | |
|---|---|
| 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. |
| Catalogue Number | 530758 |
| Brand Family | Calbiochem® |
| 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 | |
|---|---|
| References | Wu, H., et al. 2014. ACS Chem. Biol. 9, 1068. |
| Product Information | |
|---|---|
| CAS number | 1469988-75-7 |
| Form | Yellow powder |
| Hill Formula | C₂₇H₂₁N₅O₂ |
| Chemical formula | C₂₇H₂₁N₅O₂ |
| Reversible | N |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Primary Target | BMX & BTK |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Número de referencia | GTIN |
| 5307580001 | 04055977242966 |