HSP90α-IN-1
HSP90α-IN-1 is a HSP90α inhibitor (IC50 = 111 nM) that exhibits senolytic activity across various cellular senescence models. HSP90α-IN-1 is related to the xanthinic family. HSP90α-IN-1 is involved in research on combating age-related inflammaging and diseases, including cancer, and possibly extend a healthy lifespan.
For research use only. We do not sell to patients.
- CAS No.: 184897-90-3
- Formula: C19H16N4O2
- Molecular Weight:332.36
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
HSP90α 111 nM (IC50) |
HSP90α-IN-1 (Compound K5) (1 μM, 48 h) shows the highest senolytic activity on senescent cells in PD15 and PD19 cell lines while maintaining a robust level of safety for non-senescent cells[1].
HSP90α-IN-1 (1 pM-10 μM, 48 h) shows a dose-dependent inhibition against HSP90α (IC50 = 111 nM)[1].
HSP90α-IN-1 (0.1-200 μM, 48 h) shows significant senolytic effect on senescent IMR90 (PD22) (EC50 = 380 nM) and WI38 (PD51) (EC50 = 650 nM) at 500 nM with no evident toxicity[1].
HSP90α-IN-1 (25 μM, 48 h) shows apoptotic effect in senescent IMR90 cells (PD21)[1].
HSP90α-IN-1 (10 μM, 24-96 h) reduces the SA-β-gal staining in 4-hydroxytamoxifen (TAM) (HY-13757A)-treated MCF7 cell line and increases the mortality rate of senescent cells, showing senolytic effect on senescent cells (EC50 = 24.4 μM) and low cytotoxicity in proliferating cells (EC50 = 167.2 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Senescent IMR90 (PD21) cells; TAM-treated (10 μM, 96 h) MCF7 cell line
-
Concentration:25 μM (for IMR90); 10 μM (for MCF7)
-
Incubation Time:48 h (for IMR90); 24-96 h (for MCF7)
-
Result:Significantly lowered the the Pearson's Rr (PRr) coefficient of Cytochrome C (Cyt C) and mithochondria colocalization in IMR90 (PRr = 0.109) measured by CoFinder (ImageJ) compared vehicle control (PRr = 0.769) and Dasatinib (HY-10181) control (PRr = 0.643).
Significantly increased Annexin V over 96 h in MCF7 cell line.
HSP90α-IN-1 (10 μg/mL, i.p., 3 doses over 3 consecutive days) significantly reduces the senescent cell burden in P16-3MR mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Wild-type Canton-S Drosophila melanogaster (n = 884; 445 males and 439 females)[1]
-
Dosage:10 μg/mL,100 μg/mL
-
Administration:Supplement in food, alternate with vials containing only fresh food 3 times/week
-
Result:Presented a 6.63% increase in lifespan (50.69 days) compared to the controls (47.54 days).
Reduced the levels of Upd2 and Upd3 in Canton-S Drosophila melanogaster, suggesting affected JAK/STAT signaling pathway.
Demonstrated beneficial effect towards female (p=0.002) whilst male was p=0.044 when survival date were stratified by sex.
Lower dose (10 μg/mL) resulted in better survival data.
Extended lifespan when administered throughout life and when initiated in adulthood, highlighting its potential effect for late-onset intervention.
-
Animal Model:P16-3MR mice (n = 9; 4 males and 5 females), aged 26 months[1]
-
Dosage:10 μg/mL
-
Administration:Intraperitoneal injection (i.p.), 3 doses over 3 consecutive days
-
Result:Showed substantial reduction in the expression of senescence markers (p21 and p53).
Led to a decrease in SA-β-gal activity at T1.
Reduced circulating levels of two cytokines associated with the secretory profile of senescent cells (IL-6 and IL-1β) at T1 compared to T0.
Indicated no systemic toxicity and exerted positive effect in male mice.
Chemical Information
-
CAS No. 184897-90-3
-
Molecular Weight 332.36
-
Formula C19H16N4O2
-
SMILES
O=C(N1CC2=CC=CC=C2)N(C3=CC=CC=C3C)C4=C(NC=N4)C1=O
-
Shipping
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HSP90α-IN-1 Related Classifications
HY-173337 Related Classifications
Powered by Bioz