CCG-100602

Catalog No.E0345 Batch:E034501

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Technical Data

Formula

C21H17ClF6N2O2
Molecular Weight 478.82 CAS No. 1207113-88-9
Solubility (25°C)* In vitro DMSO 96 mg/mL (200.49 mM)
Ethanol 48 mg/mL (100.24 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling that acts by blocking nuclear translocation of MRTF-A with an IC50 of 10 µM.
Targets
Rho/MRTF/SRF [1]
(in RhoA/C-activated SRE-luciferase assay)
10 μM
In vitro

CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling, which blocks MRTF-A nuclear localization, thus inhibits the fibrogenic transcription factor SRF.[2]
In vivo

CCG-100602 abrogates the increase of aortic stiffness represented by reduced arterial compliance and strain inspontaneously hypertensive rat, indicating a significant anti-stiffening effect resulting from the inhibition of SRF/myocardin.[3]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Human adipose stem cell (hASC)

  • Concentrations

    3, 8, 15, or 30 μM

  • Incubation Time

    7 days

  • Method

    hASCs are cultured 7 d in basic culture medium (BM), osteogenic medium (OM), or adipogenic medium (AM) supplemented with 15, 20, 25, or 30 μM CCG-1423 or 3, 8, 15, or 30 μM CCG-100602 inhibitor, after which LIVE/DEAD analysis is performed. Green dye represents living cells, and a negligible number of dead cells are stained with red dye.
Animal Study:

[3]
  • Animal Models

    Adult (4 month-old) male spontaneously hypertensive rats (SHR) and normotensive control Wistar-Kyoto (WKY) rats

  • Dosages

    7.5 mg/kg/day

  • Administration

    osmotic minipumps

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.