GW806742X

Name: GW806742X
Brand: MedChemExpress
SKU: HY-112292
Rating: 5.0 (23 reviews)

Cat. No.: HY-112292 Purity: 99.38%: Data Sheet
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Handling Instructions
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GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a K_d of 9.3 μM. GW806742X has activity against VEGFR2 (IC₅₀=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis.

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

CAS No. : 579515-63-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of GW806742X:

GW806742X hydrochloride In-stock

23 Publications Citing Use of MCE GW806742X

Cell Proliferation/Viability Assay

IHC

In Vivo Imaging

: GW806742X purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]; WB analysis of necroptosis markers after 48 h treatment with different necroptosis inhibitors. The inhibitors used were Nec-1 (50 µM, a RIPK1 inhibitor), GSK-872 (3 µM, a RIPK3 inhibitor), and GW806742X (1 µM, an MLKL inhibitor).

: GW806742X purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]; WB analysis of PCNA in cells untreated/treated with GW806742X (1 µM) for 48 h.

: GW806742X purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]; CD47 IHC staining of primary tumours from C57BL/6 orthotopic model received different treatments: saline, anti-mouse IL6 (200 µg, iv., 3×/week), or GW806742X (100 µM in 50 µl, iv., 3×/week); mice were euthanized 4 weeks after injection.

: GW806742X purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 18;15(1):6043. [Abstract]; Bioluminescence of total tumour burden in C57BL/6 orthotopic model received different treatments: saline, GW806742X (100 µM in 50 µl, iv., 3×/week), anti-mCD47 (400 µg, ip., 3×/week) or both since day 7 after injection (106 KPC OE-MLKL cells); Images were collected at four weeks after injection; (8 mice per group).

: GW806742X purchased from MedChemExpress. Usage Cited in: Nature. 2023 Mar;615(7950):158-167. [Abstract]; Cell viability assessment in Tbk1-null B16 cells pre-treated with RIPK3 inhibitor (HS-1371, 2 μM) or MLKL inhibitor (GW806742X, 5 μM) and the pan-caspase inhibitor Q-VD-Oph (20 μM) +/− TNFα/IFNγ for 9 days (n=6, 2 independent experiments: 2-way ANOVA, Dunnett’s multiple comparisons test).

: GW806742X purchased from MedChemExpress. Usage Cited in: Autophagy. 2022 Apr;18(4):726-744. [Abstract]; Western blots for levels of p-MLKL and MLKL in wild type (WT) L929 cells untreated or treated with either TSZ for 6 h or ECS for 3 h. GW806742X (GW, 1 µM) was included in some samples as indicated 0.5 h before and during the treatment.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

MLKL

9.3 μM (Kd)

VEGFR2

2 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Fibroblast	IC₅₀	< 50 nM Compound: 42	Anti-necroptotic activity in mouse dermal fibroblast assessed as inhibition in T/S/Q induced necroptosis measured by flow cytometry Anti-necroptotic activity in mouse dermal fibroblast assessed as inhibition in T/S/Q induced necroptosis measured by flow cytometry	[PMID: 36781172]
Fibroblast	IC₅₀	< 50 nM Compound: 69; GW806742X	Anti-neprotic activity in mouse fibroblasts cells Anti-neprotic activity in mouse fibroblasts cells	[PMID: 31622096]
HUVEC	IC₅₀	5 nM Compound: 23	Inhibitory concentration against human umbilical vein endothelial cells (HUVECs) induced by VEGF Inhibitory concentration against human umbilical vein endothelial cells (HUVECs) induced by VEGF	[PMID: 15990302]
Jurkat	EC₅₀	1.85 μM Compound: 42	Anti-necroptotic activity in FADD-deficient human Jurkat cells assessed as reduction in cell growth preincubated for 30 mins followed by TNFalpha stimulation incubated overnight by CellTiter-Glo assay Anti-necroptotic activity in FADD-deficient human Jurkat cells assessed as reduction in cell growth preincubated for 30 mins followed by TNFalpha stimulation incubated overnight by CellTiter-Glo assay	[PMID: 36781172]

In Vitro

GW806742X (0.1-10000 nM) inhibits necroptotic death of wild-type mouse dermal fibroblasts (MDFs) stimulated with TSQ (1 ng/mL TNF, 500 nM compound A (Smac mimetic), 10 μM Q-VD-OPh) in a dose-dependent manner^[1].
GW806742X shows inhibition of VEGF induced proliferation of HUVECs with an IC50 of 5 nM^[2].

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

Molecular Weight

573.55

Formula

C₂₅H₂₂F₃N₇O₄S

CAS No.

579515-63-2

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=CC(NC2=NC=CC(N(C)C3=CC=C(NC(NC4=CC=C(OC(F)(F)F)C=C4)=O)C=C3)=N2)=C1)(N)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (174.35 mM; Need ultrasonic; 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	1.7435 mL	8.7176 mL	17.4353 mL
5 mM	0.3487 mL	1.7435 mL	3.4871 mL
10 mM	0.1744 mL	0.8718 mL	1.7435 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.91%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (244 KB)

Handling Instructions (2659 KB)

References

[1]. Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7. [Content Brief]

[2]. Sammond DM, et al. Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. Bioorg Med Chem Lett. 2005;15(15):3519-3523. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7435 mL	8.7176 mL	17.4353 mL	43.5882 mL
	5 mM	0.3487 mL	1.7435 mL	3.4871 mL	8.7176 mL
	10 mM	0.1744 mL	0.8718 mL	1.7435 mL	4.3588 mL
	15 mM	0.1162 mL	0.5812 mL	1.1624 mL	2.9059 mL
	20 mM	0.0872 mL	0.4359 mL	0.8718 mL	2.1794 mL
	25 mM	0.0697 mL	0.3487 mL	0.6974 mL	1.7435 mL
	30 mM	0.0581 mL	0.2906 mL	0.5812 mL	1.4529 mL
	40 mM	0.0436 mL	0.2179 mL	0.4359 mL	1.0897 mL
	50 mM	0.0349 mL	0.1744 mL	0.3487 mL	0.8718 mL
	60 mM	0.0291 mL	0.1453 mL	0.2906 mL	0.7265 mL
	80 mM	0.0218 mL	0.1090 mL	0.2179 mL	0.5449 mL
	100 mM	0.0174 mL	0.0872 mL	0.1744 mL	0.4359 mL

GW806742X Related Classifications

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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:

GW806742X579515-63-2Mixed Lineage KinaseVEGFRMLKsVascular endothelial growth factor receptorTSQnecroptoticdeathHUVECmembranetranslocationInhibitorinhibitorinhibit

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GW806742X

Customer Review

Other Forms of GW806742X:

GW806742X Related Antibodies

23 Publications Citing Use of MCE GW806742X

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

GW806742X Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GW806742X Related Classifications

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