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SB-218078
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB-218078图片
CAS NO:135897-06-2
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
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。
生物活性

SB-218078 is a potent, selective, ATP-competitive and cell-permeablecheckpoint kinase 1 (Chk1)inhibitor that inhibitsChk1phosphorylation of cdc25C with anIC50of 15 nM. SB-218078 is less potently inhibitsCdc2(IC50of 250 nM) andPKC(IC50of 1000 nM). SB-218078 causesapoptosisby 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].

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].

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

性状

Solid

Formula

C24H15N3O3

CAS 号

135897-06-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month