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| | NSC 600157 Basic information |
| Product Name: | NSC 600157 | | Synonyms: | 2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione;2-(3-Pyridylmethylene)-1,3-indandione;NSC 600157;PRT4165;PRT 4165(NSC 600157);PRT 4165; PRT-4165; NSC600157; NSC-600157; NSC 600157; 2-(pyridin-3-ylmethylidene)indene-1,3-dione;1H-Indene-1,3(2H)-dione, 2-(3-pyridinylmethylene)- | | CAS: | 31083-55-3 | | MF: | C15H9NO2 | | MW: | 235.24 | | EINECS: | | | Product Categories: | | | 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 | | 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. |
| WGK Germany | 3 | | RTECS | NK6710000 |
| | 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 600157 Preparation Products And Raw materials |
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