YM-1 tosylate
Based on 1 publication(s) in Google Scholar
YM-1 tosylate is a stable MKT-077 (HY-15096) analog and an orally active Hsp70 inhibitor. YM-1 tosylate induces cell death of HeLa cells and up-regulates the level of p53 and p21 proteins.
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- CAS 番号: 1427450-47-2
- 分子式: C27H27N3O4S3
- 分子量:553.72
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 YM-1 tosylate
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生物活性
製品説明
IC50 & Target
[1]|
HSP70 3.2 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| FM3A | EC50 |
1.1 x 10-5M
Compound: 8d
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Cytotoxicity against mouse mammary tumor FM3A cells representing a model of host
Cytotoxicity against mouse mammary tumor FM3A cells representing a model of host
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[PMID: 11855978] |
体外実験
YM-1 tosylate promotes Hsp70-dependent steps in nNOS maturation and partially blocks formation of the ATP-bound form[1]. YM-1 (0-200 μM) tosylate activates the binding of Hsp70 to its unfolded substrate[1]. YM-1 (0.001-1000 μM) tosylate converts Hsp70 to its tight-affinity conformation and shows binding efficacy to Hsp70 with an IC50 value of 8.2 μM[1]. YM-1 (0, 0.1, 0.5 and 1 μM; 24 hours) tosylate promotes nNOS ubiquitination[1]. YM-1 (5 and 10 μM; 24 and 48 hours) tosylate induces cell death of HeLa cells and growth arrest of hTERT-RPE1 cells[2]. YM-1 (10 μM; 48 hours) tosylate up-regulates p53 and p21 proteins and down-regulates FoxM1 and survivin[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7, MCF10A and MDA-MB-231
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Concentration:0-30 μM
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Incubation Time:72 h
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Result:Inhibited viability with EC50s of 2.0 ± 0.2, 3.3 ± 0.3 and 5.2 ± 0.8 μM for MDA-MB-231, MCF10A and MCF7, respectively.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 mice[1]
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Dosage:20 mg/kg
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Administration:Intravenous injection (Pharmacokinetic Analysis)
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Result:Initial pharmacokinetics of HSP70-IN-4 (Compound YM-01; 20 mg/kg; i.v.)[1]
hour plasma (ng/mL) brain (ng/g) kidney (ng/g) 0.16 359 0 74378 1 324 0 63231
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Animal Model:UAS-hAR52Q flies with polyQ AR-induced dihydrotestosterone (DHT) phenotype[1]
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Dosage:1 mM
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Administration:Oral administration; 1 mM, for 7 days
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Result:Weakened the DHT-dependent eye degeneration phenotype and rescued DHT-dependent pupal toxicity of the polyQ AR.
化学情報
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CAS 番号 1427450-47-2
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分子量 553.72
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分子式 C27H27N3O4S3
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SMILES
CN(C1=CC=CC=C1S/2)C2=C3C(N(CC)/C(S\3)=C/C4=[N+](C)C=CC=C4)=O.[O-]S(=O)(C5=CC=C(C)C=C5)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)