BIX 02188
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $960 | Check With Us |
| 500mg | $1390 | Check With Us |
| 1g | $2085 | Check With Us |
: Cat #: V0457 CAS #: 334949-59-6 Purity ≥ 98%
Description: BIX02188 (BIX-02188), an indolinone analog, is a novel, highly potent and selective MEK5 inhibitor with the potential to relieve neuropathic pain.
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| Molecular Weight (MW) | 412.48 |
|---|---|
| Molecular Formula | C25H24N4O2 |
| CAS No. | 334949-59-6 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 43 mg/mL (104.2 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 3 mg/mL (7.3 mM) | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL |
| SMILES Code | CN(CC1=CC(N/C(C2=CC=CC=C2)=C3C(NC4=C3C=CC(C(N)=O)=C4)=O)=CC=C1)C |
| Synonyms | BIX-02188; BIX 02188; BIX02188 |
| Protocol | In Vitro | BIX02188 is a potent inhibitor of catalytic function of purified, active MEK5 enzyme. In activated HeLa cells, BIX02188 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, JNK and p38 MAP kinases. To characterize the effects of BIX02188 in cultured endothelial cells (EC), H2O2 is used to activate BMK1. Bovine lung microvascular endothelial cells (BLMECs) are pretreated with 0.1-10 μM BIX02188 for 30 min, and then stimulated with 300 μM H2O2. BMK1 is dramatically activated by H2O2, with peak at 20 min. Phosphorylated BMK1 is inhibited by BIX02188 in a dose-dependent manner, with an IC50=0.8±1.0 μM, and maximal inhibition at concentrations >3 μM. To examine the specificity of BIX02188, The effect of 0.1-10 μM BIX02188 is measured on the activity of ERK1/2 and JNK. There is no significant inhibition of ERK1/2 and JNK at these concentrations. These observations confirm the selectivity of BIX02188 for MEK5-induced BMK1 phosphorylation. |
|---|
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.4244 mL | 12.1218 mL | 24.2436 mL | 48.4872 mL |
| 5mM | 0.4849 mL | 2.4244 mL | 4.8487 mL | 9.6974 mL |
| 10mM | 0.2424 mL | 1.2122 mL | 2.4244 mL | 4.8487 mL |
| 20mM | 0.1212 mL | 0.6061 mL | 1.2122 mL | 2.4244 mL |
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Method for preparing in vivo formulation:
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PEG300, mix and clarify, next add
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