1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Stearoyl-CoA Desaturase (SCD)

Stearoyl-CoA Desaturase (SCD) (硬脂酰辅酶A去饱和酶)

硬脂酰辅酶 A 去饱和酶 (SCD) 是膜流动性的关键调节剂,周转迅速,是内质网 (ER) 短寿命蛋白质选择性降解的模型。SCD 是一种限速脂肪生成酶,在催化单不饱和脂肪酸(主要是油酸和棕榈油酸)合成中起着不可或缺的作用。两者都是生物膜的主要组成部分。小鼠和人类中存在多种 SCD 同工型,即分别为 SCD-1 至 SCD-4 和 SCD-1 和 SCD-5。

SCD 的过度表达是显而易见的,并且与糖尿病和非酒精性脂肪肝等代谢疾病有关。SCD 还刺激典型 Wnt 通路和 YAP 激活,以支持干细胞和肿瘤发生。SCD 促进癌症中的代谢重编程,这至少部分是通过 MUFA 调节 AKT、AMPK 和 NF-kB 介导的。从生物学角度来看,SCD1 的过度表达会导致许多代谢紊乱,包括肥胖、胰岛素抵抗、高血压和高甘油三酯血症等。SCD1 是治疗肥胖、糖尿病和其他代谢疾病的药理学靶点。

Stearoyl-CoA desaturase (SCD) is a key regulator of membrane fluidity, turns over rapidly, and represents a model for selective degradation of short-lived proteins of the endoplasmic reticulum (ER). SCD is a rate-limiting lipogenic enzyme that plays an integral role in catalyzing the synthesis of monounsaturated fatty acids, chiefly oleate and palmitoleate. Both contribute a major part of the biological membrane. Numerous SCD isoforms exist in mouse and humans, i.e., SCD-1 to SCD-4 and SCD-1 and SCD-5, respectively.

Overexpression of SCD is evident and implicated in metabolic diseases such as diabetes and non-alcoholic fatty liver disease. SCD also stimulates canonical Wnt pathway and YAP activation in support of stemness and tumorigenesis. SCD facilitates metabolic reprogramming in cancer which is mediated, at least in part, by regulation of AKT, AMPK, and NF-kB via MUFAs. From the biological viewpoint, hyperexpression of SCD1 causes many metabolic disorders including obesity, insulin resistance, hypertension, and hypertriglyceridemia, etc. SCD1 is a pharmacological target in the treatment of obesity, diabetes and other metabolic diseases.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N6807S
    Elemicin-d3

    榄香素-d3

    Inhibitor
    Elemicin-d3 是氘代标记的 Pemafibrate (HY-17618)。Pemafibrate是高度选择性的 PPARα 激动剂,EC50 为1 nM。
    Elemicin-d<sub>3</sub>
  • HY-W011197
    Cbz-L-Trp-OH

    N-Cbz-L-色氨酸

    Inhibitor 99.74%
    Cbz-L-Trp-OH是一种 SCD 竞争型抑制剂,IC50 为 2.5 μM,Ki 为 2.1 μM。
    Cbz-L-Trp-OH
  • HY-155209
    SCD1 inhibitor-5 Inhibitor
    SCD1 inhibitor-5 (compound 51) 是 SCD1 抑制剂。SCD1 inhibitor-5 对 H2122 和 H1819 细胞的 IC50 值分别为 0.13 μM 和 31 μM。SCD1 inhibitor-5 可用于癌症研究。
    SCD1 inhibitor-5
  • HY-114527
    TPMP-I-2 Inhibitor
    TPMP-I-2 是一种抗癌剂,能够诱导癌细胞系的凋亡 (Apoptosis) 并降低硬脂酰-CoA 去饱和酶 (stearoyl-CoA desaturase) 的蛋白水平。TPMP-I-2 与免疫毒素结合在模拟微转移性宫颈癌模型中延长了裸鼠的生存时间,并且在乳腺癌模型中减少了肿瘤生长。
    TPMP-I-2
  • HY-W009121
    Cbz-D-Trp-OH

    Nα-苄氧羰基-D-色氨酸

    Inhibitor
    Cbz-D-Trp-OH 是一种 SCD 竞争型抑制剂,IC50 为 86 μM,Ki 为 71 μM。
    Cbz-D-Trp-OH
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