2. Apoptosis
  3. RIP kinase
  4. PK68

PK68 是一种高效、特异性的受体相互作用激酶 1 (RIPK1) 的 II 型抑制剂，具有口服活性。其 IC50 值约 90 nM，可抑制 RIPK1 依赖性坏死。PK68 对 TNF 诱导的全身炎症反应综合征有较强的改善作用，可用于炎症紊乱和肿瘤转移的研究。

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PK68 Chemical Structure

PK68 Chemical Structure

CAS No. : 2173556-69-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1980
In-stock
1 mg ￥750
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5 mg ￥1800
In-stock
10 mg ￥2700
In-stock
25 mg ￥4590
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PK68 相关抗体

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RIPK1 RIPK2 RIPK3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis[1].

IC50 & Target

RIPK1

90 nM (IC50)

RIPK1

23 nM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-29 EC50
23 nM
Compound: 6; PK68
Anti-necroptic activity in human HT-29 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition ans measured after 24 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptic activity in human HT-29 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition ans measured after 24 hrs by celltiter-glo luminescent cell viability assay
[PMID: 34906762]
L929 EC50
13 nM
Compound: 6; PK68
Anti-necroptic activity in mouse L929 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition and measured after 24 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptic activity in mouse L929 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition and measured after 24 hrs by celltiter-glo luminescent cell viability assay
[PMID: 34906762]
体外研究
(In Vitro)

PK68 has highly potent inhibition of TNF-induced necroptosis with EC50 values of 23 nM and 13 nM in human and mouse cells, respectively[1].
PK68 is a highly selective inhibitor of RIPK1 kinase activity with IC50 value of 90 nM[1].
PK68 (100 nM, 1 h) blocks necroptosis through the suppression of RIPK3 function or signaling upstream of RIPK3 activation[1].

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

PK68 相关抗体:

Cell Viability Assay[1]

Cell Line: Bone marrow-derived macrophages, NIH3T3-RIPK3 cells
Concentration: 100 nM
Incubation Time: 1 h
Result: PK68 block cellular activation of RIPK1, RIPK3, and MLKL upon necroptotic stimuli.
PK68 inhibit TNF-induced necroptosis but not RIPK3 dimerization-induced cell death in NIH3T3-RIPK3 cells.

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 100 nM
Incubation Time: 1 h
Result: Completely abolished phosphorylation of RIPK1, RIPK3, and MLKL.

Immunofluorescence[1]

Cell Line: HT-29 cells
Concentration: 100 nM
Incubation Time: 1 h
Result: Prevented generation of RIPK3 puncta.
体内研究
(In Vivo)

PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice[1].
PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome[1].
PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis[1].

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

Animal Model: C57BL/6 mice[1]
Dosage: 5 mg/kg, 25 mg/kg
Administration: 5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days
Result: Exhibited favorable pharmacokinetic profiles and no obvious toxicity in mice treated with a 14-day course at a dose of 25 mg/kg.
Animal Model: C57BL/6 mice[1]
Dosage: 2 mg/kg, 10 mg/kg
Administration: 2 mg/kg, i.v.; 10 mg/kg, p.o; for 14 days
Result:
PO (Gavage) IV (Bolus)
Tmax (hr) 0.5
Cmax (ng/mL) 2423
AUC0-24 (ng/mL•hr) 4821 1588
AUCINF (ng/mL•hr) 4897 1590
t1/2 (hr) 1.3 1.0
MRT (hr) 1.8 0.8
CL (mL/hr/kg) 1258
CL (mL/min/kg) 21
Vss (mL/kg) 1009
Vss (L/kg) 1.0
F(%) 61
Animal Model: C57BL/6 mice[1]
Dosage: 1 mg/kg
Administration: 1 mg/kg, i.p.
Result: Provided effective protection against TNFα-induced lethal shock.
Animal Model: C57BL/6 mice[1]
Dosage: 5 mg/kg
Administration: 5 mg/kg, i.v.
Result: Significantly reduced the number of pulmonary metastasis nodules, decreased lung metastasis, decreased number of RFP-LL/2 cells, attenuated transmigration of RFP-LL/2 cells through the endothelial cell monolayer and had no obvious influence on the proliferation rate and invasion ability of B16-F10 or RFP-LL/2 cells without the endothelial cell monolayer in vitro.
分子量

424.52

Formula

C22H24N4O3S
CAS 号
性状

固体

颜色

Off-white to light yellow

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
细胞实验： 

DMSO 中的溶解度 : 30 mg/mL (70.67 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3556 mL 11.7780 mL 23.5560 mL
5 mM 0.4711 mL 2.3556 mL 4.7112 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

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

    Solubility: ≥ 3 mg/mL (7.07 mM); 澄清溶液

    此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 30.0 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。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
  • 方案 二

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

    Solubility: ≥ 2.08 mg/mL (4.90 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.92%

COA (260 KB) HNMR (228 KB) RP-HPLC (162 KB) LCMS (158 KB)

产品使用指南 (1538 KB)
参考文献

PK68 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3556 mL 11.7780 mL 23.5560 mL 58.8900 mL
5 mM 0.4711 mL 2.3556 mL 4.7112 mL 11.7780 mL
10 mM 0.2356 mL 1.1778 mL 2.3556 mL 5.8890 mL
15 mM 0.1570 mL 0.7852 mL 1.5704 mL 3.9260 mL
20 mM 0.1178 mL 0.5889 mL 1.1778 mL 2.9445 mL
25 mM 0.0942 mL 0.4711 mL 0.9422 mL 2.3556 mL
30 mM 0.0785 mL 0.3926 mL 0.7852 mL 1.9630 mL
40 mM 0.0589 mL 0.2945 mL 0.5889 mL 1.4723 mL
50 mM 0.0471 mL 0.2356 mL 0.4711 mL 1.1778 mL
60 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9815 mL
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:

PK682173556-69-7PK 68PK-68RIP kinaseReceptor-interacting protein kinasesRIPKoraltype II inhibitorreceptor-interacting kinase 1 (RIPK1)TNFinflammatorycancerInhibitorinhibitorinhibit

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