An inhibitor of the Rho/MKL1/SRF transcriptional pathway
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Product Categories

Product Type

Biochemicals

Research Area

Cancer
Cell Migration & Metastasis

CCG-203971

Item No. 15075

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide
CAS Number
1443437-74-8
Molecular Formula
C23H21ClN2O3
Formula Weight
408.9
Purity
≥90%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 25 mg/mlEthanol: 50 mg/ml
λmax
252, 281 nm
SMILES
O=C(N1CCCC(C(NC2=CC=C(Cl)C=C2)=O)C1)C3=CC(C4=CC=CO4)=CC=C3
InChi Code
InChI=1S/C23H21ClN2O3/c24-19-8-10-20(11-9-19)25-22(27)18-6-2-12-26(15-18)23(28)17-5-1-4-16(14-17)21-7-3-13-29-21/h1,3-5,7-11,13-14,18H,2,6,12,15H2,(H,25,27)
InChi Key
HERLZBNILRVHQN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $53

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    10 mg

    $98

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    25 mg

    $231

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    50 mg

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    Cayman Chemical
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    Product Description

    Signaling through small G proteins of the RhoA subfamily, including RhoC, induces actin-regulated cytosolic-to-nuclear translocation of the oncogene product megakaryoblastic leukemia 1 (MKL1), which binds to serum response factor (SRF).1 The MKL1/SRF complex, in turn, activates the transcription of serum response element (SRE) regulated genes, stimulating cell migration, a process that is central to metastasis.1 CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM.2 This compound also inhibits PC-3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay.2 CCG-203971 causes no cytotoxicity when evaluated by WST-1 assay.2 It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Evelyn, C.R., Wade, S.M., Wang, Q., et al. CCG-1423: A small-molecule inhibitor of RhoA transcriptional signaling. Mol. Cancer Ther. 6(8), 2249-2260 (2007).

    2. Bell, J.L., Haak, A.J., Wade, S.M., et al. Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents. Bioorg. Med. Chem. Lett. 23(13), 3826-3832 (2013).