SML2355

BIX02189

≥98% (HPLC)

• Synonym(s): (3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide, (Z)-3-((3-((Dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide, BIX 02189, BIX-02189
• Empirical Formula (Hill Notation): C₂₇H₂₈N₄O₂
• CAS Number: 1265916-41-3
• Molecular Weight: 440.54
• MDL番号: MFCD18074528

Properties

• アッセイ: ≥98% (HPLC)
• 形状: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: −20°C
• SMILES string: CN(C)CC1=CC=CC(N/C(C2=CC=CC=C2)=C(C3=CC=C(C(N(C)C)=O)C=C3N4)\C4=O)=C1

Description

包装

5, 25 mg

生物化学的／生理学的作用

BIX02189 is an ATP site-targeting, potent and selective MEK5 inhibitor (IC50 =1.5 nM, [ATP] = 750 nM) with much reduced or no potency against 79 other kinases (CSF1R (FMS)/ERK5/Lck/Jak3/TGFβR1/RPS6KA6 (RSK4) IC50 = 46/59/250/440/580/990 nM, MEK1/MEK2/ERK2/JNK2/EGFR/STK16 IC50 >6.2 μM). BIX02189 blocks cellular ERK5, but not ERK1/2 or p38, phosphorylation induction (IC50 <1 μM in sorbitol-stimulated HeLa), as well as downstream MEF2C transcriptional activation (IC50 = 0.53/0.26 μM, MEK5/ERK5/MEF2C HeLa/HEK293 reporter cells). BIX02189 in vivo efficacies are demonstrated in murine models of atherosclerosis, cancer, and diabetes (10-20 mg/kg i.p.).

Safety Information

• 保管分類コード: 13 - Non Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable