SB218078
- CAS No.
- 135897-06-2
- Chemical Name:
- SB218078
- Synonyms
- 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-;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
- CBNumber:
- CB51075435
- Molecular Formula:
- C24H15N3O3
- Molecular Weight:
- 393.39
- MDL Number:
- MFCD27991263
- MOL File:
- 135897-06-2.mol
- MSDS File:
- SDS
Melting point | >340 °C |
---|---|
Density | 1.80±0.1 g/cm3(Predicted) |
storage temp. | Store at RT |
solubility | ≤5mg/ml in DMSO;5mg/ml in dimethyl formamide |
form | crystalline solid |
pka | 9.75±0.20(Predicted) |
color | Light yellow to yellow |
FDA UNII | S6U3J3UP11 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H302-H315-H319-H335 |
Precautionary statements | P261-P305+P351+P338 |
SB218078 price More Price(11)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | 559402 | SB 218078 - CAS 135897-06-2 - Calbiochem | 135897-06-2 | 1mg | $223 | 2023-01-07 | Buy |
Cayman Chemical | 13335 | SB 218078 ≥98% | 135897-06-2 | 1mg | $141 | 2024-03-01 | Buy |
TRC | S155068 | SB218078 | 135897-06-2 | 2.5mg | $160 | 2021-12-16 | Buy |
ApexBio Technology | C3012 | SB218078 | 135897-06-2 | 1mg | $160 | 2021-12-16 | Buy |
ChemScene | CS-0028421 | SB-218078 ≥98.0% | 135897-06-2 | 1mg | $150 | 2021-12-16 | Buy |
SB218078 Chemical Properties,Uses,Production
Description
SB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that blocks phosphorylation of cdc25 with an IC50 value of 15 nM. It less potently inhibits cdc2 and PKC (IC50s = 250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 μM. SB 218078 releases G2 cell cycle arrest induced by γ-irradiation or the topoisomerase I inhibitor topotecan . In this way, SB 218078 enhances the cytotoxicity of DNA-damaging compounds.
Uses
SB 218078 is a selective inhibitor of Chk1.
Definition
ChEBI: LSM-1274 is an indolocarbazole.
Biological Activity
Inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC 50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G 2 cell cycle arrest caused by γ -irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.
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.SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment significantly increases the cytotoxicity of DNA damage .
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.
target
chk1, cdc2 and pkc
IC 50
15, 250 and 1000 nm for chk1, cdc2 and pkc respectively
storage
Store at RT
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.
SB218078 Preparation Products And Raw materials
Raw materials
Preparation Products
SB218078 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
3B Pharmachem (Wuhan) International Co.,Ltd. | 821-50328103-801 18930552037 | 3bsc@sina.com | China | 15848 | 69 |
Spectrum Chemical Manufacturing Corp. | 021-021-021-67601398-809-809-809 15221380277 | marketing_china@spectrumchemical.com | China | 9664 | 60 |
Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7887 | 56 |
AdooQ Bioscience CHINA | 025-58849295 18951903616; | info@adooq.cn | China | 2990 | 60 |
EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8449 | 60 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9806 | 58 |
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