2. Apoptosis
  3. RIP kinase
  4. GSK547

GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), 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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 350 In-stock
50 mg USD 550 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].

IC50 & Target

RIP1[1]
Cellular Effect
Cell Line Type Value Description References
L929 IC50
32 nM
Compound: 76
Inhibition of RIP1 in mouse L929 cells assessed as reduction in TNF/zVAD.fmk-induced necrotic death measured after 24 hrs by cell titer-glo luminescent cell viability assay
Inhibition of RIP1 in mouse L929 cells assessed as reduction in TNF/zVAD.fmk-induced necrotic death measured after 24 hrs by cell titer-glo luminescent cell viability assay
[PMID: 31013427]
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].

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

GSK547 Related Antibodies

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].

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

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.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=NC=NC(N2CCC(C(N3N=CC[C@H]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 : 175 mg/mL (441.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

  • Protocol 2

    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

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.86%

SDS (393 KB)

COA (250 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5228 mL 12.6138 mL 25.2277 mL 63.0692 mL
5 mM 0.5046 mL 2.5228 mL 5.0455 mL 12.6138 mL
10 mM 0.2523 mL 1.2614 mL 2.5228 mL 6.3069 mL
15 mM 0.1682 mL 0.8409 mL 1.6818 mL 4.2046 mL
20 mM 0.1261 mL 0.6307 mL 1.2614 mL 3.1535 mL
25 mM 0.1009 mL 0.5046 mL 1.0091 mL 2.5228 mL
30 mM 0.0841 mL 0.4205 mL 0.8409 mL 2.1023 mL
40 mM 0.0631 mL 0.3153 mL 0.6307 mL 1.5767 mL
50 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2614 mL
60 mM 0.0420 mL 0.2102 mL 0.4205 mL 1.0512 mL
80 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7884 mL
100 mM 0.0252 mL 0.1261 mL 0.2523 mL 0.6307 mL
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GSK547 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.

Keywords:

GSK5472226735-55-1GSK'547GSK 547GSK-547RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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