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  3. GSK-872

GSK-872 

目录号: HY-101872 纯度: 99.91%
产品使用指南

GSK-872 是 RIPK3 抑制剂,高亲和力结合 RIP3 激酶结构域,IC50为1.8 nM,并抑制激酶活性,IC50为1.3 nM。GSK-872 降低 RIPK3 介导的坏死 (necroptosis) 和随后的 HMGB1 的细胞质易位和表达,并改善早期脑损伤中的脑水肿和神经功能缺损。

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GSK-872 Chemical Structure

GSK-872 Chemical Structure

CAS No. : 1346546-69-7

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10 mM * 1 mL in DMSO ¥946
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5 mg ¥860
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10 mg ¥1450
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25 mg ¥2700
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100 mg ¥7800
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Customer Review

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Top Publications Citing Use of Products

    GSK-872 purchased from MCE. Usage Cited in: J Immunol. 2018 Apr 15;200(8):2826-2834.

    Wild-type BMDMs are treated with or without PM (20 μg/ml), and DMSO, Necrostatin-1 (10 μM), and GSK’872 (5 μM) as indicated, the expression of p-IkBα and p-RELA are measured by Western blot.

    GSK-872 purchased from MCE. Usage Cited in: Chin J of Oncol Prev and Treat. 2018, 10(2): 105-109.

    In the inhibitor group,GSK'872 is injected intrathecally at 30 min before model establishment; in the saline group,the same volume of saline is intrathecally injected.

    GSK-872 purchased from MCE. Usage Cited in: Transl Stroke Res. 2021 Dec;12(6):991-1017.

    Delayed administration of GSK-872 reduces the protein level of RIP3K or MLKL and GFAP after OGD/Re injury. Astrocytes are exposed to OGD for 6 h followed by reoxygenation for 24 h. GSK-872 (10 μM) is added to the cells upon reoxygenation.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury[1][2][3].

    IC50 & Target

    IC50: 1.3 nM (RIPK3)[1]

    体外研究
    (In Vitro)

    GSK-872 (GSK'872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner[1].

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

    Cell Viability Assay[1]

    Cell Line: HT-29 cells
    Concentration: 0.01, 0.03 , 0.1, 0.3, 1, and 3 μM
    Incubation Time: 24 hours
    Result: Blocked TNF-induced necroptosis in a concentration-dependent manner.
    体内研究
    (In Vivo)

    GSK-872 (25 mM; intracerebroventricular injection) can attenuate brain edema and improve neurological function following subarachnoid hemorrhage (SAH) and reduce the number of necrotic cells. GSK-872 can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein[3].

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

    Animal Model: Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model)[3]
    Dosage: 25 mM/6 μL
    Administration: Syringe pump (intracerebroventricular) at 30 min after SAH
    Result: Attenuated brain edema, improved neurological function and decreased the number of necrotic cells in the ipsilateral cortex. Decreased the expression of RIPK3, MLKL and cytoplasmic HMGB1 at 72 h after SAH in the ipsilateral cortex.
    分子量

    383.49

    Formula

    C19H17N3O2S2

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 100 mg/mL (260.76 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6076 mL 13.0381 mL 26.0763 mL
    5 mM 0.5215 mL 2.6076 mL 5.2153 mL
    10 mM 0.2608 mL 1.3038 mL 2.6076 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。-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    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.52 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,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 2.

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

      Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.52 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 25.0 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。
    参考文献

    纯度: 99.91%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    GSK-872
    目录号:
    HY-101872
    需求量: