1. Apoptosis
  2. RIP kinase
  3. GSK'481

GSK'481 (Synonyms: GSK481)

Cat. No.: HY-100131 Purity: >98.0%
Handling Instructions

GSK'481 (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). GSK'481 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.

GSK'481 Chemical Structure

GSK'481 Chemical Structure

CAS No. : 1622849-58-4

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10 mM * 1 mL in DMSO USD 91 In-stock
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100 mg USD 990 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

GSK'481 (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). GSK'481 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

GSK’481 (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].

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

GSK'481 (GSK481) inhibits Ser166 phosphorylation in three mouse RIP1 mutants (IC50=18~110 nM) more potently than in wild-type mouse[1].

Molecular Weight

377.39

Formula

C₂₁H₁₉N₃O₄

CAS No.

1622849-58-4

SMILES

O=C(C1=NOC(CC2=CC=CC=C2)=C1)N[[email protected]]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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (92.74 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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 provided by MCE.
References
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Product name:
GSK'481
Cat. No.:
HY-100131
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