947605-77-8
Chemical Structure
ERK2-IN-7
- CAS No.: 947605-77-8
- Formula:C25H29ClN4O4
- Molecular Weight:484.98
IUPAC Name: (R)-1-(2-(4-(4-acetylphenyl)piperazin-1-yl)-2-oxoethyl)-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamide
InChIKey: YPNCCYRKEHPJMN-LJQANCHMSA-N
SMILES: C(CN1C[C@H](C(NC2=CC(Cl)=C(O)C=C2)=O)CC1)(=O)N3CCN(CC3)C4=CC=C(C(C)=O)C=C4
Biological Activity: ERK2-IN-7 is an ATP-competitive ERK2 inhibitor (mouse IC50 = 0.36 μM (cERK2) and 2.6 μM (aERK2); Kd = 0.05 μM (apo ERK2) and 0.14 μM (pERK2)). ERK2-IN-7 binds both inactive and phosphorylated ERK2 and blocks MEK-mediated ERK1/2 phosphorylation through induced-fit conformational changes of the Gly-rich loop and Tyr34, thereby inhibiting p90RSK phosphorylation and proliferation in BRAF-mutant cancer cells. ERK2-IN-7 can be used for research on melanoma and colon cancer[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
ERK2-IN-7 | ERK2-IN-7 is an ATP-competitive ERK2 inhibitor (mouse IC50 = 0.36 μM (cERK2) and 2.6 μM (aERK2); Kd = 0.05 μM (apo ERK2) and 0.14 μM (pERK2)). ERK2-IN-7 binds both inactive and phosphorylated ERK2 and blocks MEK-mediated ERK1/2 phosphorylation through induced-fit conformational changes of the Gly-rich loop and Tyr34, thereby inhibiting p90RSK phosphorylation and proliferation in BRAF-mutant cancer cells. ERK2-IN-7 can be used for research on melanoma and colon cancer. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
