XMD17-109 free base

XMD17-109 is a novel, specific ERK-5 inhibitor.

For research use only. Not for human or veterinary use.

Target ERK

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

XMD17-109 structure

CAS No.: 1435488-37-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 598.00	BP-02510-500mg	In stock	Get quote
1 g	USD 998.00	BP-02510-1g	In stock	Get quote
2 g	USD 1,698.00	BP-02510-2g	In stock	Get quote
5 g	Inquire	BP-02510-5g	In stock	Inquire

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Description

XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.

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.

Identifiers

SMILES: CCOC1=C(NC2=NC=C3N(C)C(=O)C4=C(C=CC=C4)N(C4CCCC4)C3=N2)C=CC(=C1)C(=O)N1CCC(CC1)N1CCN(C)CC1
InChIKey: XVBGRTMNFNMINE-UHFFFAOYSA-N

Specifications

MW (average): 638.8022
Formula: C₃₆H₄₆N₈O₃
CAS No.: 1435488-37-1
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C 3 years; 4°C 2 years. In solvent -20°C 1 year

Solubility

Soluble in DMSO

Documents

References

[1].Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-67.

[2].Elkins, Jonathan M., et al. X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor. Journal of Medicinal Chemistry (2013), 56(11), 4413-4421.

[3].Wilhelmsen K, et al. Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. Sci Signal. 2015 Aug 25;8(391):ra86.

Same target

Search ERK

Same research area

Search Cancer