Basic information Safety Supplier Related

NSC 600157

Basic information Safety Supplier Related

NSC 600157 Basic information

Product Name:
NSC 600157
Synonyms:
  • PRT 4165; PRT-4165; NSC600157; NSC-600157; NSC 600157
  • 2-(pyridin-3-ylmethylidene)indene-1,3-dione
  • 2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione
  • 2-(3-Pyridylmethylene)-1,3-indandione
  • NSC 600157
  • PRT4165
  • PRT 4165(NSC 600157)
  • 1H-Indene-1,3(2H)-dione, 2-(3-pyridinylmethylene)-
CAS:
31083-55-3
MF:
C15H9NO2
MW:
235.24
Mol File:
31083-55-3.mol
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NSC 600157 Chemical Properties

Melting point:
154-161 °C(Solv: ethanol (64-17-5))
Boiling point:
377.63°C (rough estimate)
Density 
1.1757 (rough estimate)
refractive index 
1.6231 (estimate)
storage temp. 
2-8°C
solubility 
DMSO: soluble20mg/mL, clear
pka
3.24±0.12(Predicted)
form 
powder
color 
white to beige
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
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Safety Information

WGK Germany 
3
RTECS 
NK6710000
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NSC 600157 Usage And Synthesis

Description

PRT-4165 (31083-55-3) is an inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1). Inhibits self-ubiquitination (IC50?= 3.9 μM) but does not increase cellular levels of either subunit. Blocks Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α.1?PRT-4165 inhibits H2A/H2AX ubiquitination via blocking the E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex. Blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination?in vitro?and?in vivo?and as such represents a new tool for studying chromatin remodeling.2

Biochem/physiol Actions

PRT4165 is a potent inhibitor of PRC1 (polycomb-repressive complex 1)-mediated histone H2A ubiquitylation in vivo and in vitro. PRT4165 inhibits the in vitro histone H2A E3 ubiquitin ligase activity of PRC1 components RING1, RNF2, and a BMI1/RNF2 complex. PRT4165 also inhibits DNA double-strand breaks induced ubiquitylation of histone H2AX.

storage

Store at +4°C

References

1) Alchanati?et al. (2009),?The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex – a potentially new drug target; PLoS One,?4?e8104 2) Ismail?et al.?(2013),?A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks; J. Biol. Chem.,?288?26944

NSC 600157Supplier

Shandong Jirun Biomedical Technology Co., Ltd. Gold
Tel
0539-0539-8613587 17661611089
Email
2639273505@qq.com
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Email
isunpharm@qq.com
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Email
info@adooq.cn
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