1. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  2. STAT Apoptosis
  3. C188

C188 (CPD188) is a STAT3 inhibitor with anticancer effects. C188 inhibits STAT3 SH2/pY-peptide binding (IC50 of 20 µM against pY-peptide binding) and IL-6-mediated STAT3 phosphorylation. C188 is selective for STAT3 over STAT1. C188 inhibits nuclear-to-cytoplasmic translocation of Stat3. C188 shows highly active induces apoptosis in breast cancer cell lines with constitutive Stat3 activation (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively).

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C188 Chemical Structure

C188 Chemical Structure

CAS No. : 823828-18-8

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Description

C188 (CPD188) is a STAT3 inhibitor with anticancer effects. C188 inhibits STAT3 SH2/pY-peptide binding (IC50 of 20 µM against pY-peptide binding) and IL-6-mediated STAT3 phosphorylation. C188 is selective for STAT3 over STAT1. C188 inhibits nuclear-to-cytoplasmic translocation of Stat3. C188 shows highly active induces apoptosis in breast cancer cell lines with constitutive Stat3 activation (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively)[1].

Cellular Effect
Cell Line Type Value Description References
DU-145 GI50
21 μM
Compound: 20
Growth inhibition of human DU145 cells after 2 days by MTT assay
Growth inhibition of human DU145 cells after 2 days by MTT assay
[PMID: 22309208]
HepG2 IC50
73 μM
Compound: 39
Inhibition of IL6-mediated STAT3 phosphorylation in human HepG2 cells preincubated for 1 hr prior to IL6 challenge measured after 30 mins by immunoblot analysis
Inhibition of IL6-mediated STAT3 phosphorylation in human HepG2 cells preincubated for 1 hr prior to IL6 challenge measured after 30 mins by immunoblot analysis
[PMID: 22650325]
HT-29 GI50
4.4 μM
Compound: 20
Growth inhibition of human HT-29 cells after 2 days by MTT assay
Growth inhibition of human HT-29 cells after 2 days by MTT assay
[PMID: 22309208]
MDA-MB-468 EC50
0.73 μM
Compound: 53; C188
Induction of apoptosis in human MDA-MB-468 cells incubated for 24 hrs by ELISA assay
Induction of apoptosis in human MDA-MB-468 cells incubated for 24 hrs by ELISA assay
[PMID: 31810784]
In Vitro

C188 (CPD188) (0-300 μM; 24 h) shows preferentially induces apoptosis in cultures expressing constitutively active STAT3 (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively), while being less effective against cells without constitutively active STAT3 (EC50s of 15.5 µM and 17.19 µM in MDA-MB-453 and MCF7 cultures, respectively)[1].
C188 (1-300 µM; pretreated for 60 min, then stimulated with IL-6 (30 ng/mL) for 30 min) inhibits IL-6-mediated tyrosine phosphorylation of Stat3 in the immunoblot assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: MDA-MB-468, MDA-MB-231, MDA-MB-435, MDA-MB-453, MCF7 cells
Concentration: 0, 0.1, 0.3, 1, 3, 10, 30, 100, 300 μM
Incubation Time: 24 hours
Result: Induced apoptosis of MDA-MB-468, MDA-MB-231 and MDA-MB-435 cell lines with constitutive Stat3 activity in a dose-dependent manner.
Had detectable activity against MDA-MB-453 and MCF7 cell lines, but showed preferential activity against cell lines with constitutive Stat3 activity.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 1, 3, 10, 30, 100, 300 µM
Incubation Time: Pretreated for 60 min; then stimulated with IL-6 (30 ng/mL) for 30 min
Result:
Molecular Weight

433.45

Formula

C19H15NO7S2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)C1=CC=C(S(=O)(NC2=C3C=CC=CC3=C(O)C(SCC(O)=O)=C2)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (230.71 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3071 mL 11.5354 mL 23.0707 mL
5 mM 0.4614 mL 2.3071 mL 4.6141 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: ≥97.0%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3071 mL 11.5354 mL 23.0707 mL 57.6768 mL
5 mM 0.4614 mL 2.3071 mL 4.6141 mL 11.5354 mL
10 mM 0.2307 mL 1.1535 mL 2.3071 mL 5.7677 mL
15 mM 0.1538 mL 0.7690 mL 1.5380 mL 3.8451 mL
20 mM 0.1154 mL 0.5768 mL 1.1535 mL 2.8838 mL
25 mM 0.0923 mL 0.4614 mL 0.9228 mL 2.3071 mL
30 mM 0.0769 mL 0.3845 mL 0.7690 mL 1.9226 mL
40 mM 0.0577 mL 0.2884 mL 0.5768 mL 1.4419 mL
50 mM 0.0461 mL 0.2307 mL 0.4614 mL 1.1535 mL
60 mM 0.0385 mL 0.1923 mL 0.3845 mL 0.9613 mL
80 mM 0.0288 mL 0.1442 mL 0.2884 mL 0.7210 mL
100 mM 0.0231 mL 0.1154 mL 0.2307 mL 0.5768 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
C188
Cat. No.:
HY-112338
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