GSK2982772

Name: GSK2982772
Brand: MedChemExpress
SKU: HY-101760
Rating: 5.0 (2 reviews)

Cat. No.: HY-101760 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

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GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC₅₀ values of 16 nM and 20 nM for human and monkey RIP1, respectively.

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

GSK2982772 Chemical Structure

CAS No. : 1622848-92-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 164	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 164	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 198	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 308	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 488	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 659	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 890	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE GSK2982772

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC₅₀ values of 16 nM and 20 nM for human and monkey RIP1, respectively^[1].

IC₅₀ & Target

IC50: 16 nM (human RIP1 FP)
IC50: 20 nM (monkey RIP1 FP)
IC50: 2 μM (rat RIP1 FP)
IC50: 2.5 μM (mouse RIP1 FP)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	CC₅₀	> 50 μM Compound: 1; GSK772	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay	[PMID: 33930803]
HT-29	CC₅₀	> 50 μM Compound: GSK'772	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by celltiter-glo luminescent cell viability assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by celltiter-glo luminescent cell viability assay	[PMID: 36288088]
HT-29	EC₅₀	0.0036 μM Compound: 1; GSK772	Anti-necroptotic activity in human HT-29 cells assessed as inhibition of hTNFalpha/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay Anti-necroptotic activity in human HT-29 cells assessed as inhibition of hTNFalpha/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay	[PMID: 33930803]
HT-29	EC₅₀	3.6 nM Compound: GSK'772	Anti-necroptotic activity in TSZ induced human HT-29 cells assessed as increase in cell viability pretreated with compound followed by TSZ stimulation and measured after 16 hrs by celltiter-glo luminescent cell viability assay Anti-necroptotic activity in TSZ induced human HT-29 cells assessed as increase in cell viability pretreated with compound followed by TSZ stimulation and measured after 16 hrs by celltiter-glo luminescent cell viability assay	[PMID: 36288088]
HT-29	IC₅₀	4.1 nM Compound: 6; GSK2982772	Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity	[PMID: 29485864]

In Vitro

GSK2982772 shows more than 1,000-fold selectivity for ERK5 over a panel of over 339 kinases at 10 μM. In stimulated cellular systems,GSK2982772 is also able to reduce spontaneous production of cytokines (IL-1β and IL-6) in a concentration-dependent fashion from ulcerative colitis explant tissue in overnight incubations. GSK2982772 produces a weak concentration dependent inhibition of hERG in human embryonic kidney (HEK-293) cells, with an estimated IC₅₀ of 195 μM, and also shows a weak activation of the human Pregnane X receptor (hPXR) with an EC₅₀ of 13 μM^[1].

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

In Vivo

GSK2982772 is dosed orally 15 min prior to TNF and shows 68, 80, and 87% protection from temperature loss over 6 h, at doses of 3, 10, and 50 mg/kg, respectively. In the corresponding TNF/zVAD model, GSK2982772 shows 13, 63, and 93% protection from temperature loss over 3 h. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, GSK2982772 has low brain penetration in rat (4%) despite possessing good cell permeability (21×10^-6 cm/s)^[1].

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

Clinical Trial

Molecular Weight

377.40

Formula

C₂₀H₁₉N₅O₃

CAS No.

1622848-92-3

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=NC(CC2=CC=CC=C2)=NN1)N[C@H]3COC4=CC=CC=C4N(C)C3=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 : 250 mg/mL (662.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6497 mL	13.2485 mL	26.4971 mL
5 mM	0.5299 mL	2.6497 mL	5.2994 mL
10 mM	0.2650 mL	1.3249 mL	2.6497 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.

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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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.51 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 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.51 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.

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: 99.79%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (250 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Harris PA, et al. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261. [Content Brief]

Animal Administration
^[1]

Mice: A total of 7 mice per dose group are orally predosed with saline or GSK2982772 at doses of 3, 10, and 50 mg/kg 15 min before i.v. administration of mouse TNF (30 μg/ mouse). Temperature loss in the mice is measured by a rectal probe. The study is terminated after 6 h when the control group lost 7 °C^[1].

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

References

[1]. Harris PA, et al. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.6497 mL	13.2485 mL	26.4971 mL	66.2427 mL
	5 mM	0.5299 mL	2.6497 mL	5.2994 mL	13.2485 mL
	10 mM	0.2650 mL	1.3249 mL	2.6497 mL	6.6243 mL
	15 mM	0.1766 mL	0.8832 mL	1.7665 mL	4.4162 mL
	20 mM	0.1325 mL	0.6624 mL	1.3249 mL	3.3121 mL
	25 mM	0.1060 mL	0.5299 mL	1.0599 mL	2.6497 mL
	30 mM	0.0883 mL	0.4416 mL	0.8832 mL	2.2081 mL
	40 mM	0.0662 mL	0.3312 mL	0.6624 mL	1.6561 mL
	50 mM	0.0530 mL	0.2650 mL	0.5299 mL	1.3249 mL
	60 mM	0.0442 mL	0.2208 mL	0.4416 mL	1.1040 mL
	80 mM	0.0331 mL	0.1656 mL	0.3312 mL	0.8280 mL
	100 mM	0.0265 mL	0.1325 mL	0.2650 mL	0.6624 mL

GSK2982772 Related Classifications

Inflammation/Immunology

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:

GSK29827721622848-92-3GSK 2982772GSK-2982772RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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GSK2982772

Customer Review

GSK2982772 Related Antibodies

2 Publications Citing Use of MCE GSK2982772

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All RIP kinase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GSK2982772 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

GSK2982772 Related Classifications

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