1. MAPK/ERK Pathway Stem Cell/Wnt
  2. ERK
  3. ERK1/2 inhibitor 10

ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations.

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ERK1/2 inhibitor 10

ERK1/2 inhibitor 10 Chemical Structure

CAS No. : 3056077-07-4

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Description

ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations[1].

IC50 & Target[1]

ERK1

0.11 nM (IC50)

ERK2

0.8 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
1.16 μM
Compound: 36c
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability incubated for 24 hrs by methyl thiazolyl tetrazolium (MTT) assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability incubated for 24 hrs by methyl thiazolyl tetrazolium (MTT) assay
[PMID: 38613499]
RKO IC50
1.07 μM
Compound: 36c
Antiproliferative activity against human RKO cells assessed as cell viability incubated for 24 hrs by methyl thiazolyl tetrazolium (MTT) assay
Antiproliferative activity against human RKO cells assessed as cell viability incubated for 24 hrs by methyl thiazolyl tetrazolium (MTT) assay
[PMID: 38613499]
Molecular Weight

465.96

Formula

C23H20ClN5O2S

CAS No.
SMILES

O=C(C1=CC(C2=NC(NC3=CC=NC(C)=C3)=NC=C2Cl)=CS1)N[C@@H](C4=CC=CC=C4)CO

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
ERK1/2 inhibitor 10
Cat. No.:
HY-162460
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