A Rho/MKL1 transcriptional pathway inhibitor
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Product Type

Biochemicals

Research Area

Cancer
Cell Migration & Metastasis
Cell Signaling

CCG-100602

Item No. 10787

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)-3-piperidinecarboxamide
CAS Number
1207113-88-9
Molecular Formula
C21H17ClF6N2O2
Formula Weight
478.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 0.2 mg/ml
λmax
250 nm
SMILES
ClC(C=C1)=CC=C1NC(C(C2)CCCN2C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O)=O
InChi Code
InChI=1S/C21H17ClF6N2O2/c22-16-3-5-17(6-4-16)29-18(31)12-2-1-7-30(11-12)19(32)13-8-14(20(23,24)25)10-15(9-13)21(26,27)28/h3-6,8-10,12H,1-2,7,11H2,(H,29,31)
InChi Key
MOQCFMZWVKQBAP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding.1 CCG-100602 is a CCG-1423 analog developed for improved selectivity, potency, and attenuated cytotoxicity relative to its parent compound. CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells with an IC50 value of 9.8 µM. At 100 μM, CCG-100602 demonstrates 72% inhibition of PC-3 cell invasion into a Matrigel model of metastasis, exhibiting an efficacy:toxicity profile superior to that of CCG-1423 at 10 μM.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. Evelyn, C.R., Bell, J.L., Ryu, J.G., et al. Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423. Bioorg. Med. Chem. Lett. 20(2), 665-672 (2010).