1. Apoptosis
  2. RIP kinase
  3. GSK547

GSK547 (Synonyms: GSK'547)

Cat. No.: HY-114492 Purity: 99.33% ee.: 99.64%
Handling Instructions

GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.

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

GSK547 Chemical Structure

GSK547 Chemical Structure

CAS No. : 2226735-55-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 520 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2600 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].

IC50 & Target

RIP1[1]

In Vitro

GSK547 (0.1-100000 nM; 24 hours) pretreats L929 cells with recombinant TNFα and zVAD at various doses for 30 min, then cell death is induced with an IC50 of 32 nM after 24 hours[1].
GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM)[1].

Cell Viability Assay[1]

Cell Line: L929 cells (Mouse L-cells NCTC 929)
Concentration: 0.1 nM; 10 nM; 1000 nM; 100000 nM
Incubation Time: 24 hours
Result: Reduced viability of L929 cells after co-treatment with TNFα and zVAD with an IC50 of 32 nM.

Western Blot Analysis[1]

Cell Line: Bone marrow-derived macrophages (BMDM)
Concentration:
Incubation Time: 30 minutes
Result: Up-regulated STAT1 signaling in BMDM.
In Vivo

GSK547 (GSK′547; RIP1i) robustly targets RIP1 in vivo. RIP1 inhibition results in immunogenic macrophage differentiation in pancreatic cancer, leading to adaptive immune activation and tumor protection for pancreatic ductal adenocarcinoma (PDA)[1].
GSK547 (100 mg/kg/day; fed via food-based dosing; 15-50 days) reduces tumor burden and extends survival compared with mice treated with controls or Nec-1s[1].

Animal Model: The wild-type (WT) mice orthotopically implanted with Pdx1Cre;KrasG12D;Trp53R172H (KPC)-derived tumor cells[1]
Dosage: ~100 mg/kg
Administration: Fed via food-based dosing, daily, 15-50 days
Result: Reduced tumor burden and extended survival.
Molecular Weight

396.39

Formula

C₂₀H₁₈F₂N₆O

CAS No.

2226735-55-1

SMILES

N#CC1=NC=NC(N2CCC(C(N3N=CC[[email protected]]3C4=CC(F)=CC(F)=C4)=O)CC2)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (315.35 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5228 mL 12.6138 mL 25.2277 mL
5 mM 0.5046 mL 2.5228 mL 5.0455 mL
10 mM 0.2523 mL 1.2614 mL 2.5228 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: ≥ 2.08 mg/mL (5.25 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
GSK547
Cat. No.:
HY-114492
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