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BMX-IN-1 A cell-permeable tricyclic quinoline-acrylamide compound that potently inhibits BMX and BTK kinase activity (IC50 = 8 and 10.4nM, respectively) by covalently targeting ATP-binding site cysteine, while being less potent against TEC family kinases TEC, JAK3, BLK with the same conserved cysteine (IC50 = 175, 377, and 653nM, respectively). Only PI 3-K gamma/PIK3CG, SBK1, PIP5K2C (by ≥94% at 1uM), and TXK (by 75% at 1uM) are significantly inhibited by BMX-IN-1 in a selectivity profiling against 437 other kinase constructs. Potently inhibits the proliferation of TEL-BMX transformed Ba/F3 Ba/F3 (GI50 = 25nM), while being much less effective against TEL-BLK, TEL-JAK1, TEL-JAK2, TEL-JAK3, or TEL-TYK2E957D transformed Ba/F3 (GI50 = ≥3.64uM) or a panel of 5 prostate cancer cell lines (GI50 ≥2.46uM). Group: Biochemicals. Alternative Names: N- (2-Methyl-5- (9- (4- (methylsulfonamido) phenyl) -2-oxobenzo[h][1, 6]naphthyridin-1 (2H) -yl) phenyl) acrylamide, BMX/BTK Inhibitor, Bruton's Tyrosine Kinase Inhibitor IV, BLK Inhibitor I, BMX Inhibitor I, JAK3 Inhibitor XIII, PI 3-K Inhibitor XX, PIP5K2C Inhibitor I, SBK1 Inhibitor I, TEC Inhibitor I, TXK Inhibitor I. Grades: Highly Purified. CAS No. 1431525-23-4. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences. USBiological 4
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BMX-IN-1 BMX-IN-1 is a selective irreversible BMX inhibitor for prostate cancer. BMX-IN-1 can covalently modifies Cys496. BMX-IN-1 inhibits the proliferation of Tel-BMX-transformed Ba/F3 cells at two digit nanomolar concentrations but requires single digit micromolar concentrations to inhibit the proliferation of prostate cancer cell lines. MK2206, is able to potentiate BMX inhibitor's antiproliferation efficacy against prostate cancer cells. Uses: Designed for use in research and industrial production. Additional or Alternative Names: BMX-IN-1; BMX-IN1; BMX-IN 1. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1431525-23-3. Molecular formula: C29H24N4O4S. Mole weight: 524.6. Purity: >98%. IUPACName: N-[5-[9-[4-(methanesulfonamido)phenyl]-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamide. Canonical SMILES: C=CC(NC1=CC(N2C(C=CC3=C2C4=CC(C5=CC=C(NS(=O)(C)=O)C=C5)=CC=C4N=C3)=O)=CC=C1C)=O. Product ID: ACM1431525233. Alfa Chemistry — ISO 9001:2015 Certified. Alfa Chemistry.
BMX-IN-1 BMX-IN-1 selectively and irreversibly inhibits BMX (IC50=8nM) that is significant for ischemia-mediated arteriogenesis and lymphangiogenesis regulation. It also inhibits the proliferation of RV-1 (GI50s=2.54μM), DU-145 (GI50s=4.38μM), PC-3 (GI50s=5.37nM). Synonyms: N-[5-[9-[4-(methanesulfonamido)phenyl]-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamideBMX-IN-1; BMX-IN1; BMX-IN 1.1431525-23-3GTPL9269SCHEMBL17052523BDBM102620CS-1295; HY-80002; W-6056; CS 1295; HY 80002; W 6056; CS1295; HY80002; W6056Example 1-14 [ WO2014063054]N-[5-[9-[4-(methanesulfonamido)phenyl]. CAS No. 1431525-23-3. Molecular formula: C29H24N4O4S. Mole weight: 524.59. BOC Sciences 11
2- (4- methyl sulfonylaminophenyl) -4, 4, 5, 5-tetra methyl -1, 3, 2-dioxaborolane 2- (4- methyl sulfonylaminophenyl) -4, 4, 5, 5-tetra methyl -1, 3, 2-dioxaborolane is a reagent for the synthesis of selective irreversible BMX kinase inhibitor BMX-IN-1 with antitumor activity. Group: Biochemicals. Grades: Highly Purified. CAS No. 616880-14-9. Pack Sizes: 500mg, 1g. Molecular Formula: C13H20BNO4S, Molecular Weight: 297.18. US Biological Life Sciences. USBiological 9
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