NSC 600157
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
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.
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
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