A Rac1 and Rac3 inhibitor; inhibits Rac1 activity (IC50 = 1.1 μM); inhibits Rac3 activity (58% at 1 μM); inhibits Cdc42 activity (28% at ≥ 5 μM); increases RhoA activity (1.3-fold at ≥2 μM); increases Rac-regulated lamellipodia formation and PAK1-mediated cell migration in MDA-MB-435 cells (2-4 μM); lowers mammary fat pad tumor growth

EHop-016 – 50 mg

Brand:
Cayman
CAS:
1380432-32-5
Storage:
-20
UN-No:
Non-Hazardous - /

EHop-016 is an inhibitor of the small Rho GTPases Rac1 and Rac3.{38132} It inhibits Rac1 activity in MDA-MB-435 breast cancer cells with an IC50 value of 1.1 μM in a Rac1 activation assay.{38131} At a concentration of 1 μM, EHop-016 inhibits 58% of Rac3 activity, and it inhibits Cdc42 activity but only at higher concentrations (5-10 μM). It also increases Rho GTPase RhoA activity ~1.3-fold at concentrations greater than 2 μM. EHop-016 (2-4 μM) inhibits Rac-regulated functions in MDA-MB-435 cells, including lamellipodia formation and serine/threonine p21-activated kinase 1 (PAK1)-mediated cell migration. In a nude mouse model of breast cancer metastasis, EHop-016 (25 mg/kg) significantly lowers mammary fat pad tumor growth, metastasis, and angiogenesis.{38134} It also inhibits mutant receptor tyrosine kinase (KIT)-induced growth in systemic mastocytosis and acute myeloid leukemia (AML) cells (≥2.5 μM).{38133}  

 

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Description

A Rac1 and Rac3 inhibitor; inhibits Rac1 activity (IC50 = 1.1 μM); inhibits Rac3 activity (58% at 1 μM); inhibits Cdc42 activity (28% at ≥ 5 μM); increases RhoA activity (1.3-fold at ≥2 μM); increases Rac-regulated lamellipodia formation and PAK1-mediated cell migration in MDA-MB-435 cells (2-4 μM); lowers mammary fat pad tumor growth, metastasis, and angiogenesis in a nude mouse model of breast cancer (25 mg/kg); inhibits mutant KIT-induced growth in systemic mastocytosis and AML cells (≥2.5 μM)

Formal name: N4-(9-ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine

Synonyms: 

Molecular weight: 430.6

CAS: 1380432-32-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|GTPases||Research Area|Cell Biology|Cell Cycle||Research Area|Cell Biology|Cell Signaling|GTPases

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