CRT0044876

Modify Date: 2024-01-02 12:08:24

CRT0044876 Structure
CRT0044876 structure
 Common Name CRT0044876
CAS Number 6960-45-8 Molecular Weight 206.155
Density 1.6±0.1 g/cm3 Boiling Point 520.8±30.0 °C at 760 mmHg
Molecular Formula C9H6N2O4 Melting Point 260-261 °C
MSDS Chinese USA Flash Point 268.8±24.6 °C
Symbol GHS08
GHS08		 Signal Word Danger

 Use of CRT0044876


CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds[1].

 Names

Name 7-Nitroindole-2-carboxylic acid
Synonym More Synonyms

 CRT0044876 Biological Activity

Description CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds[1].
Related Catalog
In Vitro A key step in BER is the processing of an apurinic/apyrimidinic (AP) site intermediate by an AP endonuclease. CRT0044876 has an IC50 for inhibition of APE1 of ∼3 μM and not only inhibits AP site cleavage catalyzed by purified APE1, but also cleavage directed by APE1 in a HeLa whole cell extract. CRT0044876 inhibits the 3′-phosphoglycolate diesterase activity of APE1 with an IC50 of ∼5 μM[1]. CRT0044876 inhibits both the exonuclease and AP endonuclease activities of exonuclease III, but shows no inhibitory activity towards endonuclease IV. CRT0044876 has minimal effects on BamHI restriction endonuclease or topoisomerase I even at CRT0044876 concentrations of 100 μM[1]. At non-toxic concentrations, CRT0044876 potentiates the cytotoxicity of several DNA damaging agents, which generate damage that is repaired in the BER pathway, including some currently-used anticancer drugs. The combination of MMS and CRT0044876 leads to a synergistic increase in the level of AP sites. Consistent with CRT0044876 being a specific BER inhibitor, a strong potentiation of hmdUrd cytotoxicity is seen in CRT0044876-treated cells (HT1080 cells)[1].
References

[1]. Madhusudan S, et al. Isolation of a small molecule inhibitor of DNA base excision repair. Nucleic Acids Res. 2005;33(15):4711-4724. Published 2005 Aug 19.

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 520.8±30.0 °C at 760 mmHg
Melting Point 260-261 °C
Molecular Formula C9H6N2O4
Molecular Weight 206.155
Flash Point 268.8±24.6 °C
Exact Mass 206.032761
PSA 98.91000
LogP 2.80
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.761
Storage condition room temp

 Safety Information

Symbol GHS08
GHS08
Signal Word Danger
Hazard Statements H319-H334
Precautionary Statements P261-P305 + P351 + P338-P342 + P311
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes Xn:Harmful;
Risk Phrases R21/22;R36/37/38
Safety Phrases S36/37/39-S26-S22
RIDADR NONH for all modes of transport
HS Code 2933990090

 Synthetic Route

Ethyl 7-nitro-1H-indole-2-carboxylate structure

Ethyl 7-nitro-1...

CAS#:6960-46-9

~98%

CRT0044876 Structure

CRT0044876

CAS#:6960-45-8

Literature: Purzer Pharmaceutical Co., Ltd. Patent: EP2366687 A2, 2011 ; Location in patent: Page/Page column 8; 10 ;
7-nitro-1H-indole-2-carboxylic acid methyl ester structure

7-nitro-1H-indo...

CAS#:167027-28-3

~96%

CRT0044876 Structure

CRT0044876

CAS#:6960-45-8

Literature: LG Life Sciences Ltd. Patent: US2010/210647 A1, 2010 ; Location in patent: Page/Page column 24 ;
ethyl 2-[2-(2-nitrophenyl)hydrazinylidene]propanoate structure

ethyl 2-[2-(2-n...

CAS#:292853-66-8

~%

CRT0044876 Structure

CRT0044876

CAS#:6960-45-8

Literature: Journal of the American Chemical Society, , vol. 80, p. 4621

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles3

More Articles
TDP1 deficiency sensitizes human cells to base damage via distinct topoisomerase I and PARP mechanisms with potential applications for cancer therapy.

Nucleic Acids Res. 42(5) , 3089-103, (2014)

Base damage and topoisomerase I (Top1)-linked DNA breaks are abundant forms of endogenous DNA breakage, contributing to hereditary ataxia and underlying the cytotoxicity of a wide range of anti-cancer...

APE1- and APE2-dependent DNA breaks in immunoglobulin class switch recombination.

J. Exp. Med. 204 , 3017-3026

Antibody class switch recombination (CSR) occurs by an intrachromosomal deletion requiring generation of double-stranded breaks (DSBs) in switch-region DNA. The initial steps in DSB formation have bee...

A novel regulatory circuit in base excision repair involving AP endonuclease 1, Creb1 and DNA polymerase beta.

Nucleic Acids Res. 39 , 3156-65, (2011)

DNA repair is required to maintain genome stability in stem cells and early embryos. At critical junctures, oxidative damage to DNA requires the base excision repair (BER) pathway. Since early zebrafi...

 Synonyms

1H-Indole-2-carboxylic acid, 7-nitro-
MFCD00044720
7-Nitro-1H-indole-2-carboxylic acid
EINECS 230-154-6
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Chemsrc provides CRT0044876(CAS#:6960-45-8) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of CRT0044876 are included as well.>> amp version: CRT0044876

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