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Submit ReviewPRT 4165
说明： Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination
化学名： 2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione
纯度： ≥99% (HPLC)
生物活性 for PRT 4165
PRT 4165 is an inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1); PRT 4165 inhibits self-ubiquitination (IC50 = 3.9 μM) but does not increase cellular levels of either subunit. PRT 4165 prevents Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α (Top2α). PRT 4165 inhibits the in vitro E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex, inhibiting H2A/H2AX ubiquitination. PRT 4165 blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro.
化合物库 for PRT 4165
PRT 4165 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for PRT 4165
| 分子量 | 235.24 |
| 公式 | C15H9NO2 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 31083-55-3 |
| PubChem ID | 207893 |
| InChI Key | OMHZFEWYVFWVLI-UHFFFAOYSA-N |
| Smiles | O=C(C2=CC=CC=C2C3=O)/C3=C\C1=CC=CN=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PRT 4165
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 23.52 | 100 | |
| 1eq. HCl | 1.18 | 5 温和加热 |
制备储备液 for PRT 4165
以下数据基于产品分子量 235.24。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.25 mL | 21.25 mL | 42.51 mL |
| 5 mM | 0.85 mL | 4.25 mL | 8.5 mL |
| 10 mM | 0.43 mL | 2.13 mL | 4.25 mL |
| 50 mM | 0.09 mL | 0.43 mL | 0.85 mL |
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产品说明书 for PRT 4165
参考文献 for PRT 4165
参考文献是支持产品生物活性的出版物。
Alchanati et al (2009) The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2α cleavage complex - a potentially new drug target. PLoS One 4 e8104 PMID: 19956605
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 PMID: 23902761
If you know of a relevant reference for PRT 4165, please let us know.
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关键词: PRT 4165, PRT 4165 supplier, PRT4165, E3, ubiquitin, ligase, inhibitors, inhibits, Bmi1, Ring1A, ubiquitination, ubiquitylation, topoisomerase, 2a, Top2a, Top2alpha, Top2α, polycomb, repressive, complex, 1, PRC1, RNF2, Bmi1/RNF2, Ubiquitin, Ligases, 5047, Tocris Bioscience
5 篇 PRT 4165 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PRT 4165 的部分引用包括：
Zhu et al (2018) BMI1 regulates androgen receptor in prostate cancer independently of the polycomb repressive complex 1. Nat Commun 9 500 PMID: 29402932
Chagraoui et al (2018) SCL/TAL1 cooperates with Polycomb RYBP-PRC1 to suppress alternative lineages in blood-fated cells. Nat Commun 9 5375 PMID: 30560907
Carsten et al (2018) CBFβ-SMMHC Inhibition Triggers Apoptosis by Disrupting MYC Chromatin Dynamics in Acute Myeloid Leukemia. Cell 174 172-186.e21 PMID: 29958106
Patrick J et al (2022) Establishment of developmental gene silencing by ordered polycomb complex recruitment in early zebrafish embryos. Elife 11 PMID: 34982026
Yan et al (2019) The Polycomb Repressor Complex 1 Drives Double-Negative Prostate Cancer Metastasis by Coordinating Stemness and Immune Suppression. Cancer Cell 36 139-155.e10 PMID: 31327655
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