SB-218078

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Chk1 的有效抑制剂，可阻断 cdc25 的磷酸化，IC50 为 15 nM。

A potent inhibitor of Chk1 that blocks phosphorylation of cdc25 with IC50 of 15 nM; less potently inhibits Cdc2 and PKC (IC50=250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 uM; enhances the cytotoxicity of DNA-damaging agents.

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.SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment significantly increases the cytotoxicity of DNA damage .Cell Cycle Analysis 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 Cell Line:HeLa and HT-29 cells Concentration:500 nM, 625 nM Incubation Time:96 hours Result:Enhanced cytotoxicity of DNA damage.

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

SB 218078 | SB218078

Angiogenesis

Chk

Chk

——

——

135897-06-2

393.4

C24H15N3O3

>98% (HPLC)

——

O=C1NC(C(C2=C3N([C@@]4([H])CC[C@]5([H])O4)C6=CC=CC=C62)=C1C7=C3N5C8=CC=CC=C78)=O

5,6,7,8-tetrahydro-13H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-13,15(14H)-dione

(-20℃)

With Ice Pack

≥ 2 years