| Identification | Back Directory | [Name]
CCG-100602 | [CAS]
1207113-88-9 | [Synonyms]
CCG-100602
CCG-100602 >=98% (HPLC)
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)piperidine-3-carboxamide
3-Piperidinecarboxamide, 1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)- | [Molecular Formula]
C21H17ClF6N2O2 | [MOL File]
1207113-88-9.mol | [Molecular Weight]
478.82 |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
≤0.2mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | [form ]
powder | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
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. 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.[Cayman Chemical] | [Biological Activity]
ccg-100602 is a rho pathway inhibitor.rho, a member of the ras superfamily of small gtp-binding proteins, plays a key role in various biological processes including microtubule dynamics, gene transcription, actin cytoskeleton organization, cell cycle progression, oncogenic transformation, as well as epithelial wound repair. | [in vitro]
ccg-100602 was developed as a ccg-1423 analog for improved selectivity, potency, and attenuated cytotoxicity. it was found that ccg-100602 was able to inhibit rhoa/c-mediated and srf-driven luciferase expression in pc-3 prostate cancer cells. at 100 μm, ccg-100602 showed 72% inhibition of pc-3 cell invasion into a matrigel model of metastasis, having an superior efficacy-toxicity profile to that of ccg-1423 [1]. | [in vivo]
to evaluate whether inhibition of srf could protect podocytes from hyperglycaemia injury, daily ip administration of ccg-1423 was performed in dm rata. results showed that ccg-1423 could ameliorate proteinuria dose-dependently. ccg-1423 at 0.02 mg/kg could significantly reduce the body weight, compared with the vehicle controls. in addition, the inhibition of srf with ccg-1423 also significantly abrogated the reduction of synaptopodin expression and the induction of srf,α-sma, fsp-1 expression in renal cortex tissues [2]. | [IC 50]
9.8 μm for pc-3 prostate cancer cells | [storage]
4°C, protect from light | [References]
[1] 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. bioorganic & medicinal chemistry letters 20, 665-672 (2010).
[2] zhao l, wang x, sun l, nie h, liu x, chen z, guan g. critical role of serum response factor in podocyte epithelial-mesenchymal transition of diabetic nephropathy. diab vasc dis res. 2016 jan;13(1):81-92. |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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