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Submit ReviewRo 5-3335 is a core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Reduces leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. Also a Tat antagonist; inhibits HIV-1 replication in vitro.
Ro 5-3335 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 259.69 |
公式 | C13H10ClN3O |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 30195-30-3 |
PubChem ID | 64983 |
InChI Key | XWNMORIHKRROGW-UHFFFAOYSA-N |
Smiles | O=C1CN=C(C3=CC=CN3)C2=C(C=CC(Cl)=C2)N1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 25.96 | 100 |
以下数据基于产品分子量 259.69。 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 | 3.85 mL | 19.25 mL | 38.51 mL |
5 mM | 0.77 mL | 3.85 mL | 7.7 mL |
10 mM | 0.39 mL | 1.93 mL | 3.85 mL |
50 mM | 0.08 mL | 0.39 mL | 0.77 mL |
参考文献是支持产品生物活性的出版物。
Cunningham et al (2012) Identification of benzodiazepine Ro5-3335 as an inhibitor of CBF leukemia through quantitative high throughput screen against RUNX1-CBF beta interaction. Proc.Natl.Acad.Sci.USA 109 14592 PMID: 22912405
Cupelli et al (1995) The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter. J.Virol. 69 2640 PMID: 7884917
Okuda et al (2001) RUNX1/AML1: a central player in hematopoiesis. Int. J. Hematol. 74 252 PMID: 11721959
If you know of a relevant reference for Ro 5-3335, please let us know.
关键词: Ro 5-3335, Ro 5-3335 supplier, Ro5-3335, CBF, core, binding, factor, Leukemia, inhibitors, inhibits, runt-related, transcription, 1, RUNX1, acute, myeloid, leukemia, protein, AML1, CBFβ, CBFα, hematopoiesis, HIV-1, replication, antiviral, CBFβ-Runx1, II, CBFbeta-Runx1, inhibitor, Other, Transcription, Factors, 4694, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Ro 5-3335 的部分引用包括:
Luo et al (2016) Runt-related Transcription Factor 1 (RUNX1) Binds to p50 in Macrophages and Enhances TLR4-triggeredInflammation and Septic Shock. Journal of Biological Chemistry PMID: 27573239
Jean Y et al (2022) LY6D marks pre-existing resistant basosquamous tumor subpopulations. Nat Commun 13 7520 PMID: 36473848
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