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说明： Molecular glue; pre-mRNA splicing modulator
化学名： N1-(3-Chloro-1H-indol-7-yl)-1,4-benzenedisulfonamide
纯度： ≥98% (HPLC)
生物活性 for Indisulam
Indisulam is an acts as a molecular glue to induce proteosomal degradation of mRNA splicing factor RBM39 (also designated CAPERα, HCC1, FSAP59, and RNPC2), via binding to DCAF15. Acts as a pre-mRNA splicing modulator (SPLAMs; splicing inhibitor sulfonamides), causes aberrant pre-mRNA splicing. Suppresses proliferation of cancer cell lines. Reduces viability of HCT-116 cells (IC50 = 0.56 μM). Induces cell cycle arrest in the G1 phase in cancer cell lines. Also a high affinity carbonic anhydrase isozyme XII (hCA XII) inhibitor (Ki = 3.0-5.7 nM).
技术数据 for Indisulam
| 分子量 | 385.84 |
| 公式 | C14H12ClN3O4S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 165668-41-7 |
| PubChem ID | 216468 |
| InChI Key | SETFNECMODOHTO-UHFFFAOYSA-N |
| Smiles | NS(=O)(C1=CC=C(S(=O)(NC2=CC=CC3=C2NC=C3Cl)=O)C=C1)=O |
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 Indisulam
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 38.58 | 100 |
制备储备液 for Indisulam
以下数据基于产品分子量 385.84。 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 | 2.59 mL | 12.96 mL | 25.92 mL |
| 5 mM | 0.52 mL | 2.59 mL | 5.18 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.59 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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产品说明书 for Indisulam
参考文献 for Indisulam
参考文献是支持产品生物活性的出版物。
Han et al (2017) Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science 28 356 PMID: 28302793
Uehara et al (2017) Selective degradation of splicing factor CAPERa by anticancer sulfonamides. Nat.Chem.Biol. 13 675 PMID: 28437394
Ozawa et al (2001) E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. Eur.J.Cancer. 37 2275 PMID: 11677118
Owa et al (1999) Discovery of novel antitumor sulfonamides targeting G1 phase of the cell cycle. J.Med.Chem. 42 3789 PMID: 10508428
Di et al (2018) Function, clinical application, and strategies of Pre-mRNA splicing in cancer. Cell Death Differ. doi: 10.1038/s41418- PMID: 30464224
Vullo et al (2005) Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? Bioorg.Med.Chem.Lett. 15 963 PMID: 15686894
If you know of a relevant reference for Indisulam, please let us know.
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关键词: Indisulam, Indisulam supplier, High, affinity, carbonic, anhydrase, isozyme, XII, (hCA, XII), inhibitors, inhibits, SPLAMs, splicing, inhibitor, sulfonamides, RNAbinding, protein, 39, RBM39, antiglaucoma, Pre-mRNA, modulator, molecular, glue, Carbonic, anhydrases, DNA,, RNA, and, Protein, Synthesis, Ubiquitin, E3, Ligases, Biochemicals, Molecular, Biology, Cell, Cycle, Inhibitors, Glues, 6782, Tocris Bioscience
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该领域的文献
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。
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