- Mitsunori Miyazaki, .et al. TSC2/Rheb signaling mediates ERK-dependent regulation of mTORC1 activity in C2C12 myoblasts, FEBS Open Bio, 2017, Mar; 7(3): 424-433 PMID: 28286738
Biological Activity
BIX 02189 is a selective dual MEK5 and ERK5 (or BMK1) kinase inhibitor, with IC50 values of 1.5, 59, 580 and >6200 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively.
Targets
Target | Value |
---|---|
MEK5 | IC50: 1.5nM |
ERK5 | IC50: 59nM |
TGFβR1 | IC50: 580nM |
MEK1 | IC50: >6.2μM |
MEK2 | IC50: >6.2μM |
ERK1 | IC50: >6.2μM |
JNK2 | IC50: >6.2μM |
EGFR | IC50: >6.3μM |
STK16 | IC50: >6.3μM |
In vitro (25°C) | DMSO | 60 mg/mL heating (136.19 mM) | |
Water | <1 mg/mL (<1 mM) | ||
Ethanol | 80 mg/mL (181.59 mM) | ||
In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol | 30 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 22.7 mL | 113.51 mL | 227.01 mL |
0.5 mM | 4.54 mL | 22.7 mL | 45.4 mL |
1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
*The above data is based on the productmolecular weight 440.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Catalog Num | A10151 |
---|---|
Actions | Inhibitor |
M. Wt | 440.5 |
Formula | C27H28N4O2 |
Solubility | DMSO |
Purity | >98% |
Storage | at -20°C 3 years Powder |
CAS No. | 1094614-85-3 |
Synonyms | BIX02189, BIX-02189 |
SMILES | CN(C)CC1=CC(=CC=C1)N/C(=C\2/C3=C(C=C(C=C3)C(=O)N(C)C)NC2=O)/C4=CC=CC=C4 |
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