CID-5951923

Alias: CID5951923; CID-5951923; CID 5951923
Cat No.:V18316 Purity: ≥98%
CID-5951923 (CID5951923) is a novel and potent inhibitor of Kruppel-like factor 5 (KLF5) expression (IC50 of 603 nM) with anticancer activity.
CID-5951923 Chemical Structure CAS No.: 749872-43-3
Product category: KLF
This product is for research use only, not for human use. We do not sell to patients.
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Product Description

CID-5951923 (CID5951923) is a novel and potent inhibitor of Kruppel-like factor 5 (KLF5) expression (IC50 of 603 nM) with anticancer activity. Compound CID 5951923 was found to be specifically effective against colon cancer cells when tested in the NCI-60 panel of human cancer cell lines.

Biological Activity I Assay Protocols (From Reference)
Targets
MEK5 (IC50 = 1.5 nM); ERK5 (IC50 = 59 nM); CSF1R (FMS) (IC50 = 46 nM); LCK (IC50 = 250 nM); JAK3 (IC50 = 440 nM); TGFβR1 (IC50 = 580 nM); RPS6KA6 (RSK4) (IC50 = 990 nM); RPS6KA3 (RSK2) (IC50 = 2.1 μM); FGFR1 (IC50 = 1 μM); KIT (IC50 = 1.1 μM); ABL1 (IC50 = 2.4 μM); MAPK14 (p38 alpha) (IC50 = 3.7 μM); SRC (IC50 = 7.6 μM)
ln Vitro
CID 5951923 (1 nM-100 μM; 48 h) inhibits DLD-1 cell proliferation in a dose-dependent manner[1].
CID 5951923 (10 μM; 24 h) significantly lowers endogenous KLF5 levels in DLD-1 cells, raises pEGFFpY1068 phosphorylation levels, and suppresses EGR1[1].
CID 5951923 (10 μM) inhibits the growth of cancer cell lines, primarily in KLF5-expressing cells[1].
References

[1]. Identification of small-molecule inhibitors of the colorectal cancer oncogene Krüppel-like factor 5 expression by ultrahigh-throughput screening. Mol Cancer Ther. 2011 Nov; 10(11): 2043-51.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H18N2O7S
Molecular Weight
382.38832
Exact Mass
382.08
Elemental Analysis
C, 50.26; H, 4.74; N, 7.33; O, 29.29; S, 8.38
CAS #
749872-43-3
Related CAS #
749872-43-3
Appearance
Solid powder
SMILES
CN(C1CCS(=O)(=O)C1)C(=O)COC(=O)/C=C/C2=CC(=CC=C2)[N+](=O)[O-]
InChi Key
URVRJYLSUVXWBC-AATRIKPKSA-N
InChi Code
InChI=1S/C16H18N2O7S/c1-17(14-7-8-26(23,24)11-14)15(19)10-25-16(20)6-5-12-3-2-4-13(9-12)18(21)22/h2-6,9,14H,7-8,10-11H2,1H3/b6-5+
Chemical Name
[2-[(1,1-dioxothiolan-3-yl)-methylamino]-2-oxoethyl] (E)-3-(3-nitrophenyl)prop-2-enoate
Synonyms
CID5951923; CID-5951923; CID 5951923
HS Tariff Code
2934.99.03.00
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~88 mg/mL (~199.8 mM)
Ethanol: ~88 mg/mL(~199.8 mM)
Solubility (In Vivo)
2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 10mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6151 mL 13.0757 mL 26.1513 mL
5 mM 0.5230 mL 2.6151 mL 5.2303 mL
10 mM 0.2615 mL 1.3076 mL 2.6151 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • Western blot and cell viability analyses of CID 5951923 and its two derivatives, CIDs 469301037 and 469301043, on DLD-1 cells. (A) Chemical structures of CIDs 5951923, 469301037, and 469301043. Mol Cancer Ther . 2011 Nov;10(11):2043-51.
  • Cell viability and KLF5 inhibition assays performed in DLD-1 cells. For the cell viability assay, DLD-1 cells were seeded in 96-well plates with medium containing DMSO or increasing concentrations of the compounds: CIDs 439501 (A) and 5951923 (B), for 2 d before the measurement of luciferase with Cell-Titer Glo assays. Mol Cancer Ther . 2011 Nov;10(11):2043-51.
  • Cell viability assays of DLD-1 and IEC-6 cells treated with the same compounds assayed in Figure 2. Cells were seeded in 96-well plates with medium containing DMSO or increasing concentrations of CIDs 4283428 (A), 439501 (B), 2567894 (C), 5951923 (D) and 4877095 (E), for 2 d before the measurement of luciferase activity with Cell-Titer Glo assays. Mol Cancer Ther . 2011 Nov;10(11):2043-51.
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