2. Cell Cycle/DNA Damage TGF-beta/Smad Epigenetics Apoptosis
  3. Checkpoint Kinase (Chk) CDK PKC Apoptosis
  4. SB-218078

SB-218078 是一种有效的，选择性，ATP 竞争性且细胞可渗透的检查点激酶 1 (Chk1) 抑制剂，可抑制 cdc25C 的 Chk1 磷酸化，IC50 为 15 nM。SB-218078 对 Cdc2 (IC50 为 250 nM) 和 PKC (IC50 为 1000 nM) 的抑制作用较弱。SB-218078 通过 DNA 损伤和细胞周期停滞诱导细胞凋亡。

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SB-218078 Chemical Structure

SB-218078 Chemical Structure

CAS No. : 135897-06-2

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1 mg ￥1380
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Customer Review

SB-218078 相关抗体

Top Publications Citing Use of Products

查看 Checkpoint Kinase (Chk) 亚型特异性产品:

查看所有亚型
Chk1 Chk2

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

查看 PKC 亚型特异性产品:

查看所有亚型
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest[1][2][3].

IC50 & Target[1]

Chk1

15 nM (IC50)

Cdc2

250 nM (IC50)

PKC

1000 nM (IC50)

Apoptosis

 

体外研究
(In Vitro)

SB-218078 (2.5-5 μM; 18 hours; HeLa cells) treatment abrogates G2 cell cycle arrest caused by either γ-irradiation or a topoisomerase I Topotecan inhibition[1].
SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment significantly increases the cytotoxicity of DNA damage [1].

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

SB-218078 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 2.5 μM, 5 μM
Incubation Time: 18 hours
Result: Abrogated G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition.

Cell Cytotoxicity Assay[1]

Cell Line: HeLa and HT-29 cells
Concentration: 500 nM, 625 nM
Incubation Time: 96 hours
Result: Enhanced cytotoxicity of DNA damage.
体内研究
(In Vivo)

SB-218078 (5 mg/kg; intraperitoneal injection; for 16 hours; C57/Bl6 mice) treatment could promote a strong increase of γ-H2AX and apoptosis throughout the lymphoma, while having no effect on a healthy spleen in Myc-induced lymphomas mouse model[2].

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

Animal Model: C57/Bl6 mice injected with ARF-/- lymphomas[2]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; for 16 hours
Result: Promoted a strong increase of γ-H2AX and apoptosis throughout the lymphoma.
分子量

393.39

Formula

C24H15N3O3
CAS 号
性状

固体

颜色

Light yellow to 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
In Vitro: 

DMSO 中的溶解度 : 40 mg/mL (101.68 mM; 超声加热助溶; 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 2.5420 mL 12.7100 mL 25.4201 mL
5 mM 0.5084 mL 2.5420 mL 5.0840 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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥98.0%

COA (185 KB) 元素分析报告 (224 KB)

产品使用指南 (1538 KB)
参考文献

SB-218078 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 2.5420 mL 12.7100 mL 25.4201 mL 63.5502 mL
5 mM 0.5084 mL 2.5420 mL 5.0840 mL 12.7100 mL
10 mM 0.2542 mL 1.2710 mL 2.5420 mL 6.3550 mL
15 mM 0.1695 mL 0.8473 mL 1.6947 mL 4.2367 mL
20 mM 0.1271 mL 0.6355 mL 1.2710 mL 3.1775 mL
25 mM 0.1017 mL 0.5084 mL 1.0168 mL 2.5420 mL
30 mM 0.0847 mL 0.4237 mL 0.8473 mL 2.1183 mL
40 mM 0.0636 mL 0.3178 mL 0.6355 mL 1.5888 mL
50 mM 0.0508 mL 0.2542 mL 0.5084 mL 1.2710 mL
60 mM 0.0424 mL 0.2118 mL 0.4237 mL 1.0592 mL
80 mM 0.0318 mL 0.1589 mL 0.3178 mL 0.7944 mL
100 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6355 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:

SB-218078135897-06-2SB218078SB 218078Checkpoint Kinase (Chk)CDKPKCApoptosisCyclin dependent kinaseProtein kinase CChk1phosphorylationcdc25CCdc2G2cyclearrestDNA-damagingapoptosisInhibitorinhibitorinhibit

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目录号：
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