SB218078
- Product Name
- 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-
- CBNumber
- CB51075435
- Molecular Formula
- C24H15N3O3
- Formula Weight
- 393.39
- MOL File
- 135897-06-2.mol
SB218078 Property
- 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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 559402
- Product name
- SB 218078 - CAS 135897-06-2 - Calbiochem
- Packaging
- 1mg
- Price
- $223
- Updated
- 2023/01/07
- Product number
- 13335
- Product name
- SB 218078
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $141
- Updated
- 2024/03/01
- Product number
- S155068
- Product name
- SB218078
- Packaging
- 2.5mg
- Price
- $160
- Updated
- 2021/12/16
- Product number
- CS-0028421
- Product name
- SB-218078
- Purity
- ≥98.0%
- Packaging
- 1mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- C3012
- Product name
- SB218078
- Packaging
- 1mg
- Price
- $160
- Updated
- 2021/12/16
SB218078 Chemical Properties,Usage,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
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