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XMD17-109

Cat. No. M4819
XMD17-109 Structure
Synonym:

ERK5-IN-1

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 120  USD120 In stock
2mg USD 50  USD50 In stock
5mg USD 90  USD90 In stock
10mg USD 170  USD170 In stock
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Quality Control & Documentation
Biological Activity

ERK5-IN-1 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 μM in HEK293 cells. The pAP1-luciferase reporter and pRL-CMV-Renilla plasmids were co-transfected with plasmids encoding for ERK5 and constitutively active MEK5 (MEK5DD) in HEK293 cells. Cells were treated with the indicated amounts of compound 26 (XMD17-109) for 24 h, and lysates were subjected to the dual-luciferase assay. Compound 26 completely inhibited the ERK5-mediated AP1 transcriptional activity at 30 μM and had an EC50 of 4.2 ± 0.7 μM.

Chemical Information
Molecular Weight 638.8
Formula C36H46N8O3
CAS Number 1435488-37-1
Solubility (25°C) DMSO ≥ 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ying Wang, et al. Cortistatin exerts antiproliferation and antimigration effects in vascular smooth muscle cells stimulated by Ang II through suppressing ERK1/2, p38 MAPK, JNK and ERK5 signaling pathways

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Keywords: XMD17-109, ERK5-IN-1 supplier, ERK, inhibitors, activators


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