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GYY4137 STAT inhibitor

Name: GYY4137
Brand: Selleck Chemicals
SKU: S9920
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S9920

GYY4137 is a novel, water-soluble hydrogen sulfide (H2S)–releasing molecule with vasodilator and antihypertensive activity. This compound shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. It also shows anti-inflammatory activity.Stock solutions should be stored under nitrogen, sealed.

Chemical Structure

Molecular Weight: 376.47

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Quality Control

Batch: Purity: 99.56%

99.56

Related Targets	EGFR JAK Pim
Other STAT Inhibitors	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 Nifuroxazide HO-3867

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (199.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 25 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.750mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.750mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	376.47	Formula	C₁₁H₁₆NO₂PS₂.C₄H₉NO	Storage (From the date of receipt)	3 years -20°C powder, oxygen-free (long-term storage)
CAS No.	106740-09-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=CC=C(C=C1)[P](S)(=S)N2CCOCC2.C3COCCN3

Mechanism of Action

Targets/IC₅₀/Ki	STAT3
In vitro	GYY4137 (400-800 µM) causes concentration-dependent killing of seven different human cancer cell lines (HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS) but does not affect survival of normal human lung fibroblasts (IMR90, WI-38).
In vivo	In the complete Freund's adjuvant (CFA)-treated mouse, GYY4137 injected 1 hr prior to CFA increased knee joint swelling while an anti-inflammatory effect, as demonstrated by reduced synovial fluid myeloperoxidase (MPO) and N-acetyl-β-D-glucosaminidase (NAG) activity and decreased TNF-α, IL-1β, IL-6 and IL-8 concentration, is apparent when this compound was injected 6 hrs after CFA.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18443240/ [2] https://pubmed.ncbi.nlm.nih.gov/24535538/ [3] https://pubmed.ncbi.nlm.nih.gov/23356870/ [4] https://pubmed.ncbi.nlm.nih.gov/21701688/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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