| 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 | [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 | [form ]
powder | [pka]
3.24±0.12(Predicted) | [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. | [InChI]
InChI=1S/C15H9NO2/c17-14-11-5-1-2-6-12(11)15(18)13(14)8-10-4-3-7-16-9-10/h1-9H | [InChIKey]
OMHZFEWYVFWVLI-UHFFFAOYSA-N | [SMILES]
C1(=O)C2=C(C=CC=C2)C(=O)/C/1=C/C1=CC=CN=C1 |
| 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 | [Uses]
PRT4165 is a potent inhibitor of polycomb-repressive complex 1 (PRC1)-mediated H2A ubiquitylation. | [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 |
|
| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
D&C Chemicals
|
| Telephone: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
|