SR18662

SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis.

SR18662  Chemical Structure

SR18662 Chemical Structure

CAS: 2505001-62-5

Selleck's SR18662 has been cited by 1 publication

Purity & Quality Control

Batch: S890001 DMSO] 84 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.77%
99.77

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Choose Selective KLF Inhibitors

Biological Activity

Description SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis.
Targets
KLF5 [1]
(Cell-free assay)
4.4 nM
In vitro
In vitro

Treatment with SR18662 significantly reduces growth and proliferation of CRC cells. SR18662 shows improved efficacy in reducing viability of multiple CRC cell lines. Flow cytometry analysis following SR18662 treatment shows an increase in cells captured in either S or G2/M phases of the cell cycle and a significant increase in the number of apoptotic cells. SR18662 treatment also reduces the expression of cyclins and components of MAPK and WNT signaling pathways.[1]

Cell Research Cell lines DLD-1, HCT116, HT29 and SW620 colorectal cancer cell lines
Concentrations 0.001 μM-20 μM
Incubation Time 24 h
Method

KLF5 promoter activity assay: DLD-1/pGL4.18hKLF5p cells are seeded in 96 well plate format and treated with DMSO or with SR18662 dissolved in DMSO in the range of 0.001 to 20 μM final concentration for 24 h and the human KLF5 promoter activity is determined with the ONE-Glo luciferase assay system using a SpectramMax M3 plate reader.

In Vivo
In vivo

A significant dose-dependent inhibition of xenograft growth in mice is observed following SR18662 treatment that exceeds the effect of ML264 at equivalent doses. SR18662 is potential for colorectal cancer therapy.[1]

Animal Research Animal Models 7-week-old male NuJ/Foxn1nu mice with DLD-1 human colorectal cells injected
Dosages 5 mg/kg, 10 mg/kg, 25 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 420.31 Formula

C16H19Cl2N3O4S

CAS No. 2505001-62-5 SDF --
Smiles C[S](=O)(=O)N1CCN(CC1)C(=O)CNC(=O)/C=C/C2=CC(=C(Cl)C=C2)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (199.85 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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