SB 218078

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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。

CAS NO:

135897-06-2

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议

产品介绍

SB 218078 是一种有效的、选择性的、ATP 竞争性和细胞可渗透的检查点激酶 1 (Chk1) 抑制剂，抑制 cdc25C 的 Chk1 磷酸化，IC5\u200b\u200b0 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引起细胞凋亡。

Cas No.	135897-06-2
化学名	9,10,11,12-tetrahydro-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione
Canonical SMILES	O=C(NC1=O)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5C7OC(CC7)N4C8=C3C=CC=C8
分子式	C₂₄H₁₅N₃O₃
分子量	393.4
溶解度	≤5mg/ml in DMSO;5mg/ml in dimethyl formamide
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Targets:Chk1, cdc2 and PKC IC50:15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively SB 218078 is a potent inhibitor of checkpoint kinase 1, with the IC50 values of 15, 250 and 1000 nM for Chk1, cdc2 and PKC, respectively. In Vitro: An in vitro kinase assay found that SB 218078 could potently inhibit the phosphorylation of Chk1, with the IC50 of 15 nM. In Hela cells, SB 218078 could cause complete abrogation of G2 cell cycle arrest induced by topotecan, with the minimum concentration of 2.5 μM [1]. Besides, 15 nM SB 218078 could effectively inhibit NKG2D ligand upregulation induced by aphidicolin in fibroblasts [2]. Furthermore, treated GM02188 cells with 2.5 μM SB 218078 could inhibit the formation of HU-induced 53bp1 foci and prevent recovery from replication fork stalling induced by APH [3]. In Vivo: In Myc-induced lymphomas mouse model, treatment with SB 218078 with the dose of 5 mg/kg could promote a strong increase of γ-H2AX and apoptosis throughout the lymphoma, while having no effect on a healthy spleen [4]. Clinical trial: No data available recently References: [1] Jackson J R, Gilmartin A G, Imburgia C S, et al. An Indolocarbazole Inhibitor of Human Checkpoint Kinase (Chk1) Abrogates Cell Cycle Arrest Caused by DNA Damage[J]. Cancer Research, 2000, 60(3): 566-572. [2] Gasser S, Orsulic S, Brown E J, et al. The DNA damage pathway regulates innate immune system ligands of the NKG2D receptor[J]. Nature, 2005, 436(7054): 1186-1190. [3] Alderton G K, Galbiati L, Griffith E, et al. Regulation of mitotic entry by microcephalin and its overlap with ATR signalling[J]. Nature Cell Biology, 2006, 8(7): 725-733. [4] Murga M, Campaner S, Lopez-Contreras A J, et al. Exploiting oncogene-induced replicative stress for the selective killing of Myc-driven tumors[J]. Nature structural & molecular biology, 2011, 18(12): 1331-1335.