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SB-218078

Catalog No. T16848 CAS 135897-06-2

SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 inhibitor that inhibits Chk1 phosphorylation of cdc25C (IC50: 15 nM).

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SB-218078, CAS 135897-06-2

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Purity: 98%

Biological Description

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Description	SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 inhibitor that inhibits Chk1 phosphorylation of cdc25C (IC50: 15 nM).
Targets&IC50	Chk1:15 nM, cdc2:250 nM, PKC:1000 nM, Apoptosis:
In vitro	SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment obviously enhances the cytotoxicity of DNA damage. 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].
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 [2].

Molecular Weight	393.39
Formula	C24H15N3O3
CAS No.	135897-06-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Jackson JR, et al. An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage. Cancer Res. 2000 Feb 1;60(3):566-72. 2. Murga M, et al. Exploiting oncogene-induced replicative stress for the selective killing of Myc-driven tumors. Nat Struct Mol Biol. 2011 Nov 27;18(12):1331-1335. 3. Preet R, et al. Chk1 inhibitor synergizes quinacrine mediated apoptosis in breast cancer cells by compromising the base excision repair cascade. Biochem Pharmacol. 2016 Apr 1;105:23-33.

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Buddlejasaponin IV VER-00158411 SB-218078 Myriocin CCT244747 CHK-IN-1 CHK1 inhibitor CHK1-IN-4 hydrochloride

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Keywords

SB-218078 135897-06-2 表观遗传细胞骨架细胞周期 Chk PKC SB 218078 SB218078 Inhibitor inhibitor inhibit

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