2. Vitamin D Related/Nuclear Receptor Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. Androgen Receptor c-Myc Akt mTOR ERK PDK-1 PI3K Apoptosis
  4. DHRS11-IN-1

DHRS11-IN-1 是一种短链脱氢酶/还原酶 SDR 家族成员 11 (DHRS11) 抑制剂，其 IC50 值为 0.037 μM。DHRS11-IN-1 可与 DHRS11 结合，与该酶的 His210 残基形成氢键。DHRS11-IN-1 可抑制雄激素受体的 mRNA 和蛋白表达，降低 c-Myc 表达，并抑制癌细胞增殖。DHRS11-IN-1 可通过降低 PDK1、AKT、mTOR 和 ERK 的磷酸化水平来抑制 PI3K/AKT 信号通路。DHRS11-IN-1 可增强 Capivasertib (HY-15431) 诱导的细胞毒性与细胞凋亡 (apoptosis)。DHRS11-IN-1 可用于管腔雄激素受体阳性三阴性乳腺癌的相关研究。

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DHRS11-IN-1

DHRS11-IN-1 Chemical Structure

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DHRS11-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DHRS11-IN-1 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC50 values of 0.037 μM. DHRS11-IN-1 binds to DHRS11, forming a hydrogen bond with the enzyme’s His210 residue. DHRS11-IN-1 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. DHRS11-IN-1 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. DHRS11-IN-1 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. DHRS11-IN-1 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer[1].

体外研究
(In Vitro)

DHRS11-IN-1 (Compound WH23)可强效抑制野生型 DHRS11，其 IC50 为 0.037 ± 0.0079 μM；且其结合能力高度依赖与 DHRS11 的 His210 形成氢键，这一点可通过其对 His210Ala 突变体的活性下降 24 倍得到证明 (IC50 = 0.87 μM)[1]。
DHRS11-IN-1 以 1.7 nM 的 IC50 值抑制 CBR1，且对 DHRS1 表现出 46 倍的选择性 [1]。
DHRS11-IN-1 (10 μM; 2-72 h) 可通过降低 AR mRNA 及蛋白水平、抑制 11KAdione (HY-135794) 诱导的 c-Myc 表达并阻断雄激素驱动的细胞生长，从而抑制 MDA-MB-453 细胞中的雄激素信号通路及细胞增殖[1]。
DHRS11-IN-1 (10 μM; 0.5-3 h) 可通过降低包括 PDK1、AKT、mTOR 和 ERK 在内的关键通路蛋白的磷酸化水平，抑制 MDA-MB-453 细胞中的 PI3K/AKT 和 MAPK 信号通路[1]。
DHRS11-IN-1 (5-20 μM; 48 h) 可选择性降低 AR 阳性 MDA-MB-453 三阴性乳腺癌细胞的活力，而对 AR 阴性 MDA-MB-231 细胞的影响极小[1]。
DHRS11-IN-1 (2-10 μM; 48 h) 可协同增强 Capivasertib (HY-15431) 对 Capivasertib 耐药 MDA-MB-453 细胞的细胞毒性与凋亡诱导作用，且小于 1 的联合指数 (combination index) 值证实了这种协同效应[1]。

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

DHRS11-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-453 cells
Concentration: 10 μM
Incubation Time: 0.5, 1, or 3 h
Result: Reduced phosphorylation of ERK (MAPK pathway), and decreased phosphorylation of PDK1, AKT, and mTOR (PI3K/AKT pathway).

Cell Viability Assay[1]

Cell Line: MDA-MB-453 (AR-positive, LAR subtype) and MDA-MB-231 (AR-negative, non-LAR subtype) triple-negative breast cancer cells
Concentration: 5, 10, 20 μM
Incubation Time: 48 h
Result: Significantly reduced viability of MDA-MB-453 cells at concentrations of 5, 10, 15, and 20 μM, but had minimal impact on viability of MDA-MB-231 cells.
分子量

326.30

Formula

C18H14O6
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

DHRS11-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

DHRS11-IN-1Androgen Receptorc-MycAktmTORERKPDK-1PI3KApoptosisMycPKBProtein kinase BMammalian target of RapamycinExtracellular signal regulated kinases3-Phosphoinositide-dependent protein kinase 1Phosphoinositide 3-kinaseMDA-MB-231 cellsMDA-MB-453 cells11-ketodihydrotestosteroneHis210DHRS11PI3K/AKT signalingluminal androgen receptor-positive triple-negative breast cancerandrogen receptorCBR1Inhibitorinhibitorinhibit

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目录号：
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