1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. MEK
    ERK

BIX02188 

Cat. No.: HY-12055 Purity: 98.80%
Handling Instructions

BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.

For research use only. We do not sell to patients.

BIX02188 Chemical Structure

BIX02188 Chemical Structure

CAS No. : 334949-59-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 179 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 163 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 307 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 931 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1675 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.

IC50 & Target[2]

MEK5

4.3 nM (IC50)

ERK5

810 nM (IC50)

CSF1R (FMS)

280 nM (IC50)

LCK

390 nM (IC50)

KIT

550 nM (IC50)

TGFβR1

1.8 μM (IC50)

ABL1

2.1 μM (IC50)

RPS6KA6 (RSK4)

3.2 μM (IC50)

RPS6KA3 (RSK2)

4.1 μM (IC50)

MAPK14 (p38 alpha)

3.9 μM (IC50)

JAK3

7.8 μM (IC50)

SRC

8.9 μM (IC50)

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[1]. BIX02188 inhibits MEK5 and ERK5 activity, with IC50s of 4.3 nM and 810 nM, respectively. BIX02188 does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2. BIX02188 inhibits ERK5 phosphorylation in a dose dependent manner[2]. To assess the proliferation of podocytes in response to the pro-fibrotic stimulus of TGFβ1, podocytes are pre-incubated in the presence and absence of BIX02188 (10 μM) for 60 min after which cells are co-treated with TGFβ1 (2.5 ng/mL) for 48 h to provide adequate time for proliferation to occur and a colorimetric cell proliferation assay is employed where metabolic activity is directly proportional to cell number. Inhibition of Erk5 activation with BIX02188 incubation reduces podocyte cell number. TGFβ1 stimulation increases podocyte cell number which is prevented following BIX02188 co-treatment[3].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.4244 mL 12.1218 mL 24.2436 mL
5 mM 0.4849 mL 2.4244 mL 4.8487 mL
10 mM 0.2424 mL 1.2122 mL 2.4244 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[3]

Human podocyte cell lines are treated at 37°C with the growth factor TGFβ1 (2.5 ng/mL in serum-free media containing BSA (0.1% w/v)). Inhibitors are applied at 37°C in serum-free media. To diminish Erk5 activation the upstream activator Mek5 is chemically inhibited by BIX02188 (10 μM) with an additional 60 min pre-incubation. TGFβ1-mediated signaling is stopped with SB431542 (10 μM), targeting the type I TGFβ receptor Alk5, with a further 30 min pre-incubation. Transmembrane receptor-induced Ras function is prevented with an additional 30 min pre-incubation using farnesylthiosalicylic acid (FTS; 10 μM). Controls (vehicles) are treated with serum-free media containing DMSO (0.1% v/v) and BSA (0.1% w/v)[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

412.48

Formula

C₂₅H₂₄N₄O₂

CAS No.

334949-59-6

SMILES

O=C(N)C1=CC(NC2=O)=C(/C2=C(C3=CC=CC=C3)/NC4=CC=CC(CN(C)C)=C4)C=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 45 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.80%

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Product Name:
BIX02188
Cat. No.:
HY-12055
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