2. NF-κB Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage Autophagy Apoptosis Immunology/Inflammation
  3. Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy
  4. Rosolutamide

Rosolutamide  (Synonyms: ASC-JM17; ALZ-003)

Cat. No.: HY-149127 Purity: ≥98.0%
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Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma.

For research use only. We do not sell to patients.

Rosolutamide

Rosolutamide Chemical Structure

CAS No. : 1039760-91-2

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Based on 1 publication(s) in Google Scholar

Rosolutamide Related Antibodies

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Description

Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma[1][2][3][4].

IC50 & Target

HSF1

 

Cellular Effect
Cell Line Type Value Description References
Glioblastoma cell line IC50
2 μM
Compound: 34; ALZ003
Induction of ferroptosis in human primary glioblastoma cells assessed as decrease in GPX4 protein expression incubated for 48 hrs by Western blot analysis
Induction of ferroptosis in human primary glioblastoma cells assessed as decrease in GPX4 protein expression incubated for 48 hrs by Western blot analysis
[PMID: 36332549]
U-87MG ATCC IC50
< 5 μM
Compound: 34; ALZ003
Induction of ferroptosis in human U-87 MG cells assessed as decrease in GPX4 protein expression incubated for 48 hrs by Western blot analysis
Induction of ferroptosis in human U-87 MG cells assessed as decrease in GPX4 protein expression incubated for 48 hrs by Western blot analysis
[PMID: 36332549]
In Vitro

Rosolutamide (0.2-5 μM; 0-12 h) accelerates UPS-mediated clearance of wild-type and polyglutamine-expanded androgen receptor in healthy control and SBMA fibroblasts, reducing AR steady-state levels and half-life[1].
Rosolutamide (5 μM) inhibits the transcriptional activity of wild-type and polyglutamine-expanded androgen receptor in DHT-treated PC12 cells[1].
Rosolutamide (0-40 μM) potently activates the heat shock response pathway in PC12 cells[1].
Rosolutamide (0-7.5 μM) activates Nrf1 to increase expression of multiple proteasome subunits in PC12 and MCF7 cells[1].
Rosolutamide enhances chymotrypsin-like, trypsin-like, and caspase-like proteasome catalytic activities in PC12 cells[1].
Rosolutamide (0-7.5 μM) activates Nrf2 to increase expression of antioxidant enzymes HO-1, Nqo1, Gclc, and catalase in PC12 cells without inducing global oxidative protein damage[1].
Rosolutamide (2.5 μM; 16 h) protects MCF7 cells against hydrogen peroxide-induced oxidative stress via Nrf2 activation[1].
Rosolutamide (0-7.5 μM) activates Hsf1 to increase expression of heat shock proteins Hsp25, Hsp40, Hsp72, Hsp90, and co-chaperone Hop in PC12 and MCF7 cells[1].
Rosolutamide (0.3-5 µM; 24 h) shows no cytotoxicity in WT, MJD26, and MJD78 cells, but induces cytotoxicity at concentrations greater than 5 µM in WT and MJD78 cells[3].
Rosolutamide (0.3-5 µM; 24 h) improves mitochondrial respiration function in MJD78 cells[3].
Rosolutamide (0.3-5 µM; 24 h) reduces mutant ataxin-3 protein expression and protein aggregation in MJD78 cells via induction of autophagy, with no effect on ATXN3 mRNA levels[3].
Rosolutamide (0.3-5 µM; 24 h) reduces oxidative stress in MJD78 cells by lowering total and mitochondrial ROS levels, and enhances antioxidant defenses by increasing NQO1, HO-1, SOD2, GSH, and catalase, with 1 µM showing the strongest effects[3].
Rosolutamide (0.3-5 µM; 24 h) activates Nrf2 in a dose-dependent manner in MJD78 cells, increasing Nrf2 transcriptional activity[3].

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

Rosolutamide Related Antibodies

Western Blot Analysis[1]

Cell Line: Healthy control fibroblasts, SBMA fibroblasts, PC12 cells
Concentration: 0.5; 1; 2; 2.5; 5 μM
Incubation Time: 0; 2; 4; 6; 8; 12 h
Result: Reduced steady-state levels of both normal and polyglutamine-expanded AR variants in the presence and absence of DHT.
Was effective at lower concentrations than ASC-J9 for reducing mutant AR protein.
Significantly reduced the half-life of polyglutamine-expanded AR compared to DMSO vehicle.
Induced ubiquitylation of both wild-type and mutant AR.
Promoted proteasome-mediated clearance of AR, which was blocked by epoxomicin.

Cell Viability Assay[3]

Cell Line: wild-type SK-N-SH human neuroblastoma cells, SK-N-SH cells stably expressing ataxin-3 with 26 CAG repeats (MJD26), SK-N-SH cells stably expressing ataxin-3 with 78 CAG repeats (MJD78)
Concentration: 0.3; 1; 5 µM
Incubation Time: 24 h
Result: Caused no cytotoxicity in WT, MJD26, or MJD78 cells at 0.3, 1, or 5 µM after 24 h.
Increased cytotoxicity in WT and MJD78 cells at concentrations >5 µM after 24 h.

Cell Autophagy Assay[3]

Cell Line: MJD78 human neuroblastoma cells
Concentration: 0.3; 1; 5 µM
Incubation Time: 24 h
Result: Had no significant effect on ATXN3 mRNA levels in MJD78 cells.
Reduced protein aggregation and mutant ataxin-3 protein expression, while upregulating p62 and LC3 II protein expression in MJD78 cells at 0.3 µM and 1 µM.
In Vivo

Rosolutamide (50 nM; incorporated into fly food; continuous exposure throughout development/ adulthood) rescues mutant AR-induced toxicity in Drosophila SBMA models, and this protective effect requires the Nrf1/Nrf2 ortholog CncC but not Hsf1[1].
Rosolutamide (120 mg/kg; i.g.; daily; 6 weeks or 16 weeks) ameliorates disease manifestations, reduces mutant AR accumulation, and activates Nrf1/Nrf2 pathways in symptomatic AR97Q mice[1].

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

Animal Model: transgenic lines: GMR:UAS-AR52Q, Elav-GAL4/UAS-AR52Q/Cyo-GFP (expressing full-length human AR with expanded polyglutamine tract (AR52Q) under GMR-GAL4 eye-specific driver or Elav-GAL4 pan-neuronal driver, treated with 1 mM DHT to induce toxicity)[1]
Dosage: 50 nM
Administration: incorporated into fly food; continuous exposure throughout development/ adulthood
Result: Rescued DHT-induced degenerative eye phenotype in GMR:UAS-AR52Q flies.
Significantly increased the population frequency of Elav > AR52Q flies from ~4% (DHT-only) to ~20% (DHT + ASC-JM17).
Failed to rescue the eye phenotype in CncC RNAi lines, but fully restored the eye phenotype in HSF RNAi lines.
Animal Model: F1 transgenic mice (AR97Q line, C57Bl6 × BDF1 background; male, post-disease onset at 10 weeks of age) with Spinal and bulbar muscular atrophy (SBMA)[1]
Dosage: 120 mg/kg
Administration: i.g.; daily; 6 weeks or 16 weeks
Result: Significantly rescued weight loss and improved motor function.
Ameliorated neurogenic and myogenic muscle atrophy features on H&E and NADH-stained quadriceps cross-sections.
Reduced monomeric and high molecular weight (HMW) mutant AR protein levels in quadriceps muscle.
Significantly increased mRNA expression of Nrf1 target genes (Psmb4, Psmc1, Psmd14; P < 0.01) and Nrf2 target genes (Gsr, Gsta2, Nqo1) in quadriceps muscle.
In a post hoc analysis excluding severely affected mice, increased median survival by ~10 weeks.
Molecular Weight

464.55

Formula

C28H32O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC(C=C1/C=C/C(C(C(/C=C/C2=CC(OC)=C(C=C2)OC)=O)CC3CCC3)=O)=C(C=C1)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (107.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1526 mL 10.7631 mL 21.5262 mL
5 mM 0.4305 mL 2.1526 mL 4.3052 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1526 mL 10.7631 mL 21.5262 mL 53.8155 mL
5 mM 0.4305 mL 2.1526 mL 4.3052 mL 10.7631 mL
10 mM 0.2153 mL 1.0763 mL 2.1526 mL 5.3816 mL
15 mM 0.1435 mL 0.7175 mL 1.4351 mL 3.5877 mL
20 mM 0.1076 mL 0.5382 mL 1.0763 mL 2.6908 mL
25 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1526 mL
30 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7939 mL
40 mM 0.0538 mL 0.2691 mL 0.5382 mL 1.3454 mL
50 mM 0.0431 mL 0.2153 mL 0.4305 mL 1.0763 mL
60 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8969 mL
80 mM 0.0269 mL 0.1345 mL 0.2691 mL 0.6727 mL
100 mM 0.0215 mL 0.1076 mL 0.2153 mL 0.5382 mL
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Rosolutamide Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rosolutamide1039760-91-2ASC-JM17 ALZ-003ALZ003ALZ 003ALZ-003Keap1-Nrf2Androgen ReceptorHSPMitophagyFerroptosisApoptosisReactive Oxygen Species (ROS)AutophagyHeat shock proteinsMitochondrial Autophagyataxin-3 aggregatesspinal and bulbar muscular atrophyNrf2Nrf1mutant androgen receptorspinocerebellar ataxiatemozolomide-resistant glioblastomaubiquitin-proteasome systemHsf1Huntington’s diseaseInhibitorinhibitorinhibit

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