SML4109
PDK4-IN-1
≥98% (HPLC)
别名:
1-(1-(Piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione hydrochloride, 1-[1-(4-Piperidinyl)-1H-pyrazol-4-yl]-9,10-anthracenedione hydrochloride
质量水平
方案
≥98% (HPLC)
表单
powder
储存条件
desiccated
颜色
white to beige
溶解性
H2O: 2 mg/mL, clear (Warmed)
储存温度
-10 to -25°C
SMILES字符串
Cl.[n]2(ncc(c2)c3c4c(ccc3)C(=O)c5c(cccc5)C4=O)C1CCNCC1
InChI key
ZIMLKZKPNALXKK-UHFFFAOYSA-N
生化/生理作用
Potent, orally active PDK4 inhibitor with antidiabetic and anticancer efficacy.
PDK4-IN-1 (PDK4i-8c) is a cell-penetrating anthraquinone derivative that has been identified as an allosteric inhibitor of pyruvate dehydrogenase kinase 4 (PDK4), whis is binding to its lipoamide binding site with a high affinity (IC50 = 84 nM). PDK4-IN-1 is orally available, demonstrates excellent metabolic stability, and exhibits a promising pharmacokinetic profile in rat studies. Moreover, PDK4-IN-1 substantially enhances glucose tolerance in mice with diet-induced obesity and mitigates allergic reactions in a passive cutaneous anaphylaxis mouse model. The in vivo data support its effectiveness as a potential treatment for diabetes. Additionally, PDK4-IN shows notable anticancer properties by regulating cell proliferation, transformation, and apoptosis.
PDK4-IN-1 (PDK4i-8c) is a cell-penetrating anthraquinone derivative that has been identified as an allosteric inhibitor of pyruvate dehydrogenase kinase 4 (PDK4), whis is binding to its lipoamide binding site with a high affinity (IC50 = 84 nM). PDK4-IN-1 is orally available, demonstrates excellent metabolic stability, and exhibits a promising pharmacokinetic profile in rat studies. Moreover, PDK4-IN-1 substantially enhances glucose tolerance in mice with diet-induced obesity and mitigates allergic reactions in a passive cutaneous anaphylaxis mouse model. The in vivo data support its effectiveness as a potential treatment for diabetes. Additionally, PDK4-IN shows notable anticancer properties by regulating cell proliferation, transformation, and apoptosis.
免责声明
Hygroscopic
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Mohammad Kasim Fatmi et al.
Aging cell, 22(4), e13800-e13800 (2023-02-18)
Ischemic heart disease (IHD) is the leading cause of death, with age range being the primary factor for development. The mechanisms by which aging increases vulnerability to ischemic insult are not well understood. We aim to use single-cell RNA sequencing
Dahye Lee et al.
Journal of medicinal chemistry, 62(2), 575-588 (2019-01-10)
Pyruvate dehydrogenase kinase 4 (PDK4) activation is associated with metabolic diseases including hyperglycemia, insulin resistance, allergies, and cancer. Structural modifications of hit anthraquinone led to the identification of a new series of allosteric PDK4 inhibitors. Among this series, compound 8c
PDK4-dependent hypercatabolism and lactate production of senescent cells promotes cancer malignancy.
Xuefeng Dou et al.
Nature metabolism, 5(11), 1887-1910 (2023-10-31)
Senescent cells remain metabolically active, but their metabolic landscape and resulting implications remain underexplored. Here, we report upregulation of pyruvate dehydrogenase kinase 4 (PDK4) upon senescence, particularly in some stromal cell lines. Senescent cells display a PDK4-dependent increase in aerobic
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