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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-;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
Formula Weight
393.39
MOL File
135897-06-2.mol
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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)
color 
Light yellow to yellow
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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.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
559402
Product name
SB 218078 - CAS 135897-06-2 - Calbiochem
Packaging
1mg
Price
$223
Updated
2023/01/07
Cayman Chemical
Product number
13335
Product name
SB 218078
Purity
≥98%
Packaging
1mg
Price
$141
Updated
2024/03/01
TRC
Product number
S155068
Product name
SB218078
Packaging
2.5mg
Price
$160
Updated
2021/12/16
ChemScene
Product number
CS-0028421
Product name
SB-218078
Purity
≥98.0%
Packaging
1mg
Price
$150
Updated
2021/12/16
ApexBio Technology
Product number
C3012
Product name
SB218078
Packaging
1mg
Price
$160
Updated
2021/12/16
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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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SB218078 Suppliers

China 18 Germany 1 United Kingdom 1 United States 6 Global 26
EMMX Biotechnology LLC
Tel
888-539-0666
Fax
888-539-0666
Email
info@emmx.com
Country
United States
ProdList
8447
Advantage
60
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32161
Advantage
58
Aladdin Scientific
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
52924
Advantage
58
ApexBio Technology
Tel
--
Fax
--
Email
sales@apexbt.com
Country
United States
ProdList
6251
Advantage
58
Cayman Chemical Company
Tel
--
Fax
--
Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81
MedChemExpress
Tel
--
Fax
--
Email
sales@medchemexpress.com
Country
United States
ProdList
6398
Advantage
58

135897-06-2, SB218078Related Search:

C-(9-ETHYL-9H-CARBAZOL-3-YL)-METHYLAMINE 1-(1-METHYL-1H-INDOL-4-YL)METHYLAMINE 97 SB218078 CARBAZOL-9-YL-METHANOL 1-ethyl-1H-indole-4-carbaldehyde N-METHYL-N-[(1-METHYL-1H-INDOL-5-YL)METHYL]AMINE 11,12-Dihydroindolo[2,3-a]carbazole 1-METHYL-1H-INDOLE-4-CARBALDEHYDE ARCYRIAFLAVIN A 4-AMINOMETHYLINDOLE N-Ethyl-3-carbazolecarboxaldehyde K-252C 1H-INDOLE-4-ETHANAMINE, N-METHYL-

  • 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
  • SB218078 ?SB-218078
  • 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
  • 135897-06-2