| Identification | Back Directory | [Name]
NSC 600157 | [CAS]
31083-55-3 | [Synonyms]
PRT4165
NSC 600157
PRT4165 >=98% (HPLC)
PRT 4165(NSC 600157)
2-(3-Pyridylmethylene)-1,3-indandione
2-(pyridin-3-ylmethylidene)indene-1,3-dione
2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione
1H-Indene-1,3(2H)-dione, 2-(3-pyridinylmethylene)-
PRT 4165; PRT-4165; NSC600157; NSC-600157; NSC 600157 | [Molecular Formula]
C15H9NO2 | [MDL Number]
MFCD00435709 | [MOL File]
31083-55-3.mol | [Molecular Weight]
235.24 |
| Chemical Properties | Back Directory | [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 | [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. |
| Hazard Information | Back Directory | [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 -20°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 |
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