2. Apoptosis
  3. RIP kinase
  4. GSK481

GSK481 

Cat. No.: HY-100131 Purity: 98.57%
COA Handling Instructions

GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM.

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

GSK481 Chemical Structure

GSK481 Chemical Structure

CAS No. : 1622849-58-4

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 100 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 100 In-stock
Solid
2 mg USD 72 In-stock
5 mg USD 121 In-stock
10 mg USD 187 In-stock
50 mg USD 649 In-stock
100 mg USD 1089 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

GSK481 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM[1].

IC50 & Target

IC50: 1.3 nM (RIP1), 2.8 nM (Ser166 phosphorylation in wild-type human RIP1)[1]
In Vitro

GSK481 (300 nM; 2 hours; Jurkat cells) abrogates the RIP3 up-regulation induces by both TNFa and shikonin in live and dead cells, indicating that necroptosis is in fact induced by both agents[2].

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

GSK481 Related Antibodies

Apoptosis Analysis[2]

Cell Line: Jurkat cells
Concentration: 300 nM
Incubation Time: 2 hours
Result: Increased levels of detectable apoptosis induced by TNFa and shikonin.
In Vivo

GSK481 inhibits Ser166 phosphorylation in three mouse RIP1 mutants (IC50=18~110 nM) more potently than in wild-type mouse[1].

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

377.39

Appearance

Solid

Formula

C21H19N3O4
CAS No.
SMILES

O=C(C1=NOC(CC2=CC=CC=C2)=C1)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 : ≥ 35 mg/mL (92.74 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6498 mL 13.2489 mL 26.4978 mL
5 mM 0.5300 mL 2.6498 mL 5.2996 mL
10 mM 0.2650 mL 1.3249 mL 2.6498 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.62 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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GSK481 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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

GSK4811622849-58-4GSK 481GSK-481RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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