2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Immunology/Inflammation
  3. HSP Interleukin Related
  4. HSP90α-IN-1

HSP90α-IN-1 是一种 HSP90α 抑制剂 (IC50 = 111 nM)，在多种细胞衰老模型中均表现出抗衰老活性。HSP90α-IN-1 属于黄嘌呤家族。HSP90α-IN-1 参与了对抗与年龄相关的炎症、衰老和疾病 (包括癌症) 的研究，并可能延长健康寿命。

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HSP90α-IN-1

HSP90α-IN-1 Chemical Structure

CAS No. : 184897-90-3

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HSP90α-IN-1 相关抗体

Top Publications Citing Use of Products

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

HSP90α-IN-1 (Compound K5) (1 μM, 48 小时) 对 PD15 和 PD19 细胞系中的衰老细胞表现出最高的抗衰老活性，同时对非衰老细胞保持了较高的安全性[1]。
HSP90α-IN-1 (1 pM-10 μM, 48 小时) 对 HSP90α 表现出剂量依赖性抑制作用 (IC50 = 111 nM)[1]。
HSP90α-IN-1 (0.1-200 μM，48 小时) 在 500 nM 浓度下对衰老的 IMR90 (PD22) (EC50 = 380 nM) 和 WI38 (PD51) (EC50 = 650 nM) 表现出显著的抗衰老作用，且无明显毒性[1]。
HSP90α-IN-1 (25 μM，48 小时) 在衰老的 IMR90 细胞 (PD21) 中表现出凋亡作用[1]。
HSP90α-IN-1 (10 μM，24-96 小时) 可降低 TAM (HY-13757A) 处理的 MCF7 细胞系中的 SA-β-半乳糖苷酶染色，并增加衰老细胞的死亡率，对衰老细胞具有抗衰老作用 (EC50 = 24.4 μM)，且对增殖细胞具有低细胞毒性 (EC50 = 167.2 μM)[1]。

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

HSP90α-IN-1 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

HSP90α-IN-1 (Compound K5) (10-100 μg/mL，通过食物补充，和新鲜食物每周替换 3 次) 可使野生型 Canton-S 果蝇 (n = 884)的寿命平均延长 6.63%[1]。
HSP90α-IN-1 (10 μg/mL，腹腔注射，连续3天，共3次) 显著降低了 P16-3MR 小鼠的衰老细胞负担[1]。

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.
分子量

332.36

Formula

C19H16N4O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HSP90α-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

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

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