天堂网亚洲,天天操天天搞,91视频高清,菠萝蜜视频在线观看入口,美女视频性感美女视频,95丝袜美女视频国产,超高清美女视频图片

返回ChemicalBook首頁>CAS數(shù)據(jù)庫列表>135897-06-2

135897-06-2

中文名稱 SB218078
英文名稱 SB218078
CAS 135897-06-2
分子式 C24H15N3O3
分子量 393.39
MOL 文件 135897-06-2.mol
135897-06-2 結(jié)構(gòu)式 135897-06-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T16848
英文別名
SB218078 ?SB-218078
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
9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione, 9,10,11,12-tetrahydro-
所屬類別
生物化工:抑制劑

物理化學(xué)性質(zhì)

熔點>340 °C
密度1.80±0.1 g/cm3(Predicted)
儲存條件Store at RT
溶解度≤5mg/ml in DMSO;5mg/ml in dimethyl formamide
酸度系數(shù)(pKa)9.75±0.20(Predicted)
形態(tài)結(jié)晶固體
顏色Light yellow to yellow

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
SB-218078 是一種有效的,選擇性,ATP 競爭性且細胞可滲透的檢查點激酶 1 (Chk1) 抑制劑,可抑制 cdc25C 的 Chk1 磷酸化,IC50 為 15 nM。SB-218078 對 Cdc2 (IC50 為 250 nM) 和 PKC (IC50 為 1000 nM) 的抑制作用較弱。SB-218078 通過 DNA 損傷和細胞周期停滯誘導(dǎo)細胞凋亡。
靶點

Chk1

15 nM (IC 50 )

Cdc2

250 nM (IC 50 )

PKC

1000 nM (IC 50 )

Apoptosis

體外研究

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.
體內(nèi)研究

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.
"135897-06-2" 相關(guān)產(chǎn)品信息
7570-45-8