2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Immunology/Inflammation
  3. HSP Interleukin Related
  4. 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.

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HSP90α-IN-1 Chemical Structure

HSP90α-IN-1 Chemical Structure

CAS No. : 184897-90-3

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HSP90α-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

HSP90α

111 nM (IC50)

In Vitro

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.

HSP90α-IN-1 Related Antibodies

Apoptosis Analysis[1]

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.
Parmacokinetics[1]
Species Dose SampleTime Route Indicator value
Mice 30 mg/kg 10 min p.o. Cmax 2802 ng/mL
Mice 5 mg/kg i.v. T1/2 13 min
In Vivo

HSP90α-IN-1 (Compound K5) (10-100 μg/mL, supplemented in food, alternate with vials containing only fresh food 3 times/week) results in an average increase of 6.63% in the lifespan of wild-type Canton-S Drosophila melanogaster (n = 884)[1].
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.
Molecular Weight

332.36

Formula

C19H16N4O2
CAS No.
SMILES

O=C(N1CC2=CC=CC=C2)N(C3=CC=CC=C3C)C4=C(NC=N4)C1=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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HSP90α-IN-1 Related Classifications

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Help & FAQs
  • 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:

HSP90α-IN-1184897-90-3HSPInterleukin RelatedHeat shock proteinsILHSP90αHSP90inhibitorsenolyticagingsenescenceInhibitorinhibit

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