1. Signaling Pathways
  2. Immunology/Inflammation
  3. Salt-inducible Kinase (SIK)

Salt-inducible Kinase (SIK) (盐诱导激酶)

Salt-inducible kinases (SIKs) belong to AMP-activated protein kinase (AMPK) family, and functions mainly involve in regulating energy response-related physiological processes, such as gluconeogenesis and lipid metabolism. The SIK family comprises three isoforms, namely, SIK1, SIK2, and SIK3, all of which may act as metabolic transmitters. SIKs have shown self-phosphorylation, and play an important role in regulating adrenocortical function under the stimulation of high salt or adreno-cortico-tropic-hormone (ACTH).

All three SIK family kinases are expressed broadly. SIK1 mRNA expression is regulated by multiple stimuli, including high dietary salt intake, ACTH signaling, glucagon signaling, excitable cell depolarization, and circadian rhythms. In contrast, SIK2 and SIK3 expression is constitutive in tissues in which these kinases are expressed. In humans, SIK2 and SIK3 are expressed ubiquitously, with highest SIK2 levels in adipose tissue and highest SIK3 expression in brain. In addition, these SIK family members are dysregulated in various cancers, including ovarian, breast, prostate, and lung cancers, indicating that SIKs may execute crucial roles in tumor occurrence or progression.

Salt-inducible Kinase (SIK) 相关产品 (9):

目录号 产品名 作用方式 纯度
  • HY-15776
    HG-9-91-01 Inhibitor 98.02%
    HG-9-91-01 是一种有效,选择性的盐诱导型激酶 (SIK) 抑制剂,作用于 SIK1SIK2SIK3IC50 分别为 0.92 nM,6.6 nM 和 9.6 nM。
  • HY-101147
    YKL-05-099 Inhibitor 99.76%
    YKL-05-099 是一种盐诱导型激酶 (SIK) 抑制剂。YKL-05-099 作用于SIK1SIK3,IC50 分别约为 10 和 30 nM。YKL-05-099 抑制 SIK2 的活性稍低,IC50 值为 40 nM。
  • HY-120856
    ARN-3236 Inhibitor 99.60%
    ARN-3236 是具有口服活性的盐诱导激酶2 (SIK2) 的选择性抑制剂,其对 SIK2、SIK1 和 SIK3 的 IC50 值分别为 <1 nM、21.63 nM 和 6.63.nM。具有抗肿瘤活性。
  • HY-120056
    YKL-06-061 Inhibitor 99.89%
    YKL-06-061 是有效的、选择性的盐诱导激酶 (SIK) 的二代抑制剂,其对 SIK1/2/3 的IC50 值为6.56 nM/1.77 nM/20.5 nM。
  • HY-120877
    MRT199665 Inhibitor 99.73%
    MRT199665 是一种有效的,ATP竞争性的,选择性 MARK/SIK/AMPK 抑制剂,对 MARK1/MARK2/MARK3/MARK14AMPKα1/AMPKα2SIK1/SIK2/SIK3IC50 分别为 2/2/3/2 nM,10/10 nM 和 110/12/43 nM。MRT199665 作用于 MEF2C 激活的人急性髓性白血病 (AML) 细胞,引起凋亡 (apoptosis)。MRT199665 抑制 SIK 底物 CRTC3 磷酸化 (在 S370 位点)。
  • HY-138001
    WH-4-025 Inhibitor 98.74%
    WH-4-025 是盐诱导激酶 (SIK) 的抑制剂 (WO2016023014 A2)。
  • HY-139253
    MRIA9 Inhibitor
    MRIA9 是 ATP 竞争性的、pan-SIKPAK2/3 抑制剂,其对 SIK1、SIK2 和 SIK3 的 IC50 值分别为 516 nM, 180 nM 和 127 nM。
  • HY-129141
    YKL-06-062 Inhibitor ≥98.0%
    YKL-06-062 是第二代 salt-inducible kinase (SIK) 抑制剂,其 IC50 为 2.12 nM/1.40 nM/2.86 nM。YKL-06-062 是 YKL-06-061 的结构类似物。
  • HY-N1570
    Pterosin B Inhibitor 99.08%
    Pterosin B 是一种从蕨菜 (Pteridium aquilinum) 中发现的茚满酮,是盐诱导性激酶 3 (Sik3) 信号转导的抑制剂。Pterosin B 通过抑制 Sik3 预防小鼠软骨细胞肥大和骨关节炎。
Isoform Specific Products

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