GSK-872 hydrochloride

Name: GSK-872 hydrochloride
Brand: MedChemExpress
SKU: HY-101872A
Rating: 5.0 (58 reviews)

Cat. No.: HY-101872A Purity: 99.21%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC₅₀ of 1.8 nM, and inhibits kinase activity with an IC₅₀ of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.

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

GSK-872 hydrochloride Chemical Structure

CAS No. : 2703752-81-0

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 99	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 99	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 390	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 58 publication(s) in Google Scholar

Other Forms of GSK-872 hydrochloride:

GSK-872 In-stock

55 Publications Citing Use of MCE GSK-872 hydrochloride

: GSK-872 hydrochloride purchased from MedChemExpress. Usage Cited in: Transl Stroke Res. 2021 Dec;12(6):991-1017. [Abstract]; Delayed administration of GSK-872 reduces the protein level of RIP3K or MLKL and GFAP after OGD/Re injury. Astrocytes are exposed to OGD for 6 h followed by reoxygenation for 24 h. GSK-872 (10 μM) is added to the cells upon reoxygenation.

: GSK-872 hydrochloride purchased from MedChemExpress. Usage Cited in: J Immunol. 2018 Apr 15;200(8):2826-2834. [Abstract]; Wild-type BMDMs are treated with or without PM (20 μg/ml), and DMSO, Necrostatin-1 (10 μM), and GSK’872 (5 μM) as indicated, the expression of p-IkBα and p-RELA are measured by Western blot.

: GSK-872 hydrochloride purchased from MedChemExpress. Usage Cited in: Chin J of Oncol Prev and Treat. 2018, 10(2): 105-109.; In the inhibitor group，GSK'872 is injected intrathecally at 30 min before model establishment; in the saline group，the same volume of saline is intrathecally injected.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

RIPK3

In Vitro

GSK-872 hydrochloride (0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner^[1].

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

Cell Viability Assay^[1]

Cell Line:	HT-29 cells
Concentration:	0.01, 0.03 , 0.1, 0.3, 1, and 3 μM
Incubation Time:	24 hours
Result:	Blocked TNF-induced necroptosis in a concentration-dependent manner.

In Vivo

GSK-872 hydrochloride (25 mM; intracerebroventricular injection) can attenuate brain edema and improve neurological function following subarachnoid hemorrhage (SAH) and reduce the number of necrotic cells. GSK-872 hydrochloride can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein^[3].

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

Animal Model:	Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model)^[3]
Dosage:	25 mM/6 μL
Administration:	Syringe pump (intracerebroventricular) at 30 min after SAH
Result:	Attenuated brain edema, improved neurological function and decreased the number of necrotic cells in the ipsilateral cortex. Decreased the expression of RIPK3, MLKL and cytoplasmic HMGB1 at 72 h after SAH in the ipsilateral cortex.

Molecular Weight

419.95

Formula

C₁₉H₁₈ClN₃O₂S₂

CAS No.

2703752-81-0

Appearance

Solid

Color

Yellow to brown

SMILES

O=S(C1=CC=C2N=CC=C(C2=C1)NC3=CC=C4SC=NC4=C3)(C(C)C)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (23.81 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2.5 mg/mL (5.95 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3812 mL	11.9062 mL	23.8124 mL
5 mM	0.4762 mL	2.3812 mL	4.7625 mL
10 mM	0.2381 mL	1.1906 mL	2.3812 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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: ≥ 0.21 mg/mL (0.50 mM); Clear solution

This protocol yields a clear solution of ≥ 0.21 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.1 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.

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).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

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: 99.21%

Select Batch:

Data Sheet (277 KB) SDS (0 KB)

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95. [Content Brief]

[2]. Arora D, et al. Deltamethrin induced RIPK3-mediated caspase-independent non-apoptotic cell death in rat primary hepatocytes. Biochem Biophys Res Commun. 2016 Oct 14;479(2):217-223. [Content Brief]

[3]. Chen T, et al. Inhibiting of RIPK3 attenuates early brain injury following subarachnoid hemorrhage: Possibly through alleviating necroptosis. Biomed Pharmacother. 2018;107:563-570. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.3812 mL	11.9062 mL	23.8124 mL	59.5309 mL
H₂O / DMSO	5 mM	0.4762 mL	2.3812 mL	4.7625 mL	11.9062 mL
DMSO	10 mM	0.2381 mL	1.1906 mL	2.3812 mL	5.9531 mL
	15 mM	0.1587 mL	0.7937 mL	1.5875 mL	3.9687 mL
	20 mM	0.1191 mL	0.5953 mL	1.1906 mL	2.9765 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.