1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. HSP
  3. YM-1 tosylate

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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YM-1 tosylate Chemical Structure

YM-1 tosylate Chemical Structure

CAS No. : 1427450-47-2

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Description

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[1][2].

IC50 & Target[1]

HSP70

3.2 μM (IC50)

In Vitro

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.

Cell Viability Assay[1]

Cell Line: MCF7, MCF10A and MDA-MB-231
Concentration: 0-30 μM
Incubation Time: 72 h
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.
In Vivo

YM-1 (1 mM; oral administration, for 7 days) tosylate rescues polyQ toxicity in Drosophila by activating Hsp70[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD1 mice[1]
Dosage: 20 mg/kg
Administration: Intravenous injection (Pharmacokinetic Analysis)
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
Animal Model: UAS-hAR52Q flies with polyQ AR-induced dihydrotestosterone (DHT) phenotype[1]
Dosage: 1 mM
Administration: Oral administration; 1 mM, for 7 days
Result: Weakened the DHT-dependent eye degeneration phenotype and rescued DHT-dependent pupal toxicity of the polyQ AR.
Molecular Weight

553.72

Formula

C27H27N3O4S3

CAS No.
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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
YM-1 tosylate
Cat. No.:
HY-18406
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