1. Apoptosis
  2. RIP kinase
  3. GSK547

GSK547 (Synonyms: GSK'547)

目录号: HY-114492 纯度: 99.74% ee.: 99.81%
产品使用指南

GSK547 (GSK'547) 是一种高效的选择性 receptor-interacting serine/threonine protein kinase 1 (RIP1) 抑制剂,可抑制巨噬细胞介导的胰腺癌适应性免疫耐受。

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GSK547 Chemical Structure

GSK547 Chemical Structure

CAS No. : 2226735-55-1

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1308 In-stock
5 mg ¥1500 In-stock
10 mg ¥2550 In-stock
25 mg ¥5100 In-stock
50 mg ¥8500 In-stock
100 mg ¥13500 In-stock
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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[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 : 100 mg/mL (252.28 mM; Need ultrasonic)

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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    此方案可获得 ≥ 2.08 mg/mL (5.25 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

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

    此方案可获得 ≥ 2.5 mg/mL (6.31 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定溶至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

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

    此方案可获得 ≥ 2.08 mg/mL (5.25 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
References

Purity: 99.74% ee.: 99.81%

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The molarity calculator equation

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

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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:

GSK547GSK'547GSK 547GSK-547RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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HY-114492
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