C188 (Synonyms: CPD188)

Name: C188
Brand: MedChemExpress
SKU: HY-112338
Rating: 4.5 (1 reviews)

Cat. No.: HY-112338 Purity: 98.29%: Data Sheet
SDS

COA
Handling Instructions
FAQs
Technical Support

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).

For research use only. We do not sell to patients.

C188 Chemical Structure

CAS No. : 823828-18-8

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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STAT3 STAT5 STAT6 STAT1

Biological Activity
Purity & Documentation
References
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Description

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.

823828-18-8

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
10 mM	0.2307 mL	1.1535 mL	2.3071 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.29%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (257 KB) HNMR (316 KB) RP-HPLC (261 KB)

Handling Instructions (2659 KB)

References

[1]. Xu X, Kasembeli MM, Jiang X, Tweardy BJ, Tweardy DJ. Chemical probes that competitively and selectively inhibit Stat3 activation. PLoS One. 2009;4(3):e4783. [Content Brief]

Complete Stock Solution Preparation Table

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

C188 Related Classifications

Help & FAQs

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.

Keywords:

C188823828-18-8CPD188C 188C-188CPD 188CPD-188STATApoptosisInhibitorinhibitorinhibit

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C188 (Synonyms: CPD188)

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C188 Related Antibodies

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Complete Stock Solution Preparation Table

C188 Related Classifications

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