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Submit ReviewFuramidine dihydrochloride is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 9.4 μM). Exhibits selectivity over PRMT5, PRMT6 and CARM1 (IC50 values are 166, 283 and >400 μM respectively). Inhibits tyrosyl-DNA phosphodiesterase 1 (TDP-1) (IC50 = 1.2 μM). Inhibits cell proliferation in leukemia cell lines, suppresses neuroblastoma tumor growth, and reduces mis-splicing in in vitro and in vivo models of myotonic dystrophy type 1. Also shows dose-dependent inhibition of platelet aggregation (IC50 = 14.8 uM). Cell-permeable.
Furamidine dihydrochloride 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。
分子量 | 377.27 |
公式 | C18H16N4O.2HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 55368-40-6 |
PubChem ID | 462428 |
InChI Key | VXNYQUQHOUERTR-UHFFFAOYSA-N |
Smiles | NC(C(C=C3)=CC=C3C1=CC=C(C2=CC=C(C(N)=N)C=C2)O1)=N.Cl.Cl |
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 | |||
water | 18.86 | 50 | |
DMSO | 18.86 | 50 |
以下数据基于产品分子量 377.27。 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 |
---|---|---|---|
0.5 mM | 5.3 mL | 26.51 mL | 53.01 mL |
2.5 mM | 1.06 mL | 5.3 mL | 10.6 mL |
5 mM | 0.53 mL | 2.65 mL | 5.3 mL |
25 mM | 0.11 mL | 0.53 mL | 1.06 mL |
参考文献是支持产品生物活性的出版物。
Yan et al (2014) Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J.Med.Chem. 57 2611 PMID: 24564570
Jenquin et al (2018) Furamidine rescues myotonic dystrophy type I associated mis-splicing through multiple mechanisms. ACS Chem.Biol. 13 2708 PMID: 30118588
Hua et al (2020) PRMT1 promotes neuroblastoma cell survival through ATF5. Oncogenesis 9 50 PMID: 32415090
Marsden et al (2021) Inhibition of arginine methylation impairs platelet function. ACS Pharmacol.Transl.Sci. 4 1567 PMID: 34661075
If you know of a relevant reference for Furamidine dihydrochloride, please let us know.
关键词: Furamidine dihydrochloride, Furamidine dihydrochloride supplier, Selective, protein, arginine, methyltransferase, 1, PRMT1, inhibitors, inhibits, leukemia, coactivator-associated, tdp1, tyrosyl, DNA, topoisomerase, Protein, Arginine, Methyltransferases, Phosphodiesterases, 5202, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Furamidine dihydrochloride 的部分引用包括:
Samuel et al (2018) Inhibiting Arginine Methylation as a Tool to Investigate Cross-Talk with Methylation and Acetylation Post-Translational Modifications in a Glioblastoma Cell Line. Proteomes 6 44 PMID: 30347783
Jer-Yen et al (2022) PRMT1 is an important factor for medulloblastoma cell proliferation and survival. Biochem Biophys Rep 32 101364 PMID: 36237442
Tang et al (2022) A genome-scale CRISPR screen reveals PRMT1 as a critical regulator of androgen receptor signaling in prostate cancer. Cell Rep. 38 110417 PMID: 35196489
Min-Jung et al (2020) TC-E 5003, a protein methyltransferase 1 inhibitor, activates the PKA-dependent thermogenic pathway in primary murine and human subcutaneous adipocytes. FEBS Lett 594 2923-2930 PMID: 32767856
Marsden et al (2021) Inhibition of Arginine Methylation Impairs Platelet Function. ACS Pharmacol.Transl.Sci 4 1567 PMID: 34661075
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.