2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein
  3. Cathepsin Cholecystokinin Receptor
  4. CLIK-148

CLIK-148 是一种高选择性、不可逆的、口服有效的半胱氨酸蛋白酶 (cysteine protease) 抑制剂，主要靶向组织蛋白酶 L (Cathepsin L)。CLIK-148 可有效抑制内质网 (ER) 膜上依赖 Cathepsin L 的 HMG-CoA 还原酶降解。CLIK-148 抑制 Cathepsin L 参与的前胆囊收缩素 (proCCK) 加工过程，减少 CCK8 (HY-P0093) 的生成。CLIK-148 阻断破骨细胞分泌的 Cathepsin L 对 Ⅰ 型胶原的降解，减少肿瘤诱导的骨转移和恶性高钙血症。CLIK-148 可用于骨代谢紊乱和神经肽加工调控的研究。

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CLIK-148

CLIK-148 Chemical Structure

CAS No. : 215098-90-1

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CLIK-148 相关抗体

Top Publications Citing Use of Products

查看 Cathepsin 亚型特异性产品:

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Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

查看 Cholecystokinin Receptor 亚型特异性产品:

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CCKAR CCKBR

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing[1][2][3][4].

IC50 & Target[1]

cathepsin L

 

体外研究
(In Vitro)

CLIK-148 (100 nM-10 μM) 在大鼠肝脏中浓度为 100 nM 时，可强效且特异性地抑制组织 Cathepsin L 活性，而浓度为 1 μM 时几乎对组织 Cathepsin B 和 C 无抑制作用，浓度为 10 μM 时仅对组织 Cathepsin S 和 K 有微弱的抑制作用[1]。
CLIK-148 (50 μM，24 小时) 可抑制组织 Cathepsin L 的活性，从而阻断 proCCK 生成 CCK9，最终减少垂体 AtT-20 细胞中 CCK8 的产生[2]。
CLIK-148 (1-10 nM, 72 小时) 可有效抑制由 TNF-α 激活的人和小鼠破骨细胞介导的骨胶原降解[3]。
CLIK-148 (100 μM) 可有效保护 HMG-CoA 还原酶免于在 C100 细胞坏死性损伤的情况下发生病理性降解[4]。

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

CLIK-148 相关抗体:
体内研究
(In Vivo)

CLIK-148 (1-10 mg/kg，腹腔注射，单次给药) 显著抑制小鼠肝脏中的组织蛋白酶 L，同时对组织蛋白酶 B 的活性完全没有影响[1]。
CLIK-148 (50 mg/kg，口服，每日一次，共 7 天) 可有效预防和治疗小鼠肿瘤引起的恶性高钙血症[3]。
CLIK-148 (32-128 mg/kg，口服或静脉注射，每日一次，共 7 天) 可有效抑制结肠癌细胞的直接骨转移和局部骨破坏[3]。
CLIK-148 (100-200 mg/kg，口服，每日一次，共 14 天) 可特异性抑制癌细胞通过血液转移到骨骼的过程在小鼠中[3]。

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

Animal Model: Mice model[1]
Dosage: 1, 3 and 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Specifically targeted and inhibited Cathepsin L in the lysosomes of the liver dose-dependently, while having no effect on Cathepsin B.
Animal Model: LJC-1 cells induced direct bone metastasis and local bone resorption model of cancer established in mice[3]
Dosage: 5 mg/kg
Administration: Oral administration (p.o.), once daily for 7 days
Result: Significantly reduced the serum calcium level in mice.
Animal Model: Colon tumor 26 PMF-15 cells induced hypercalcemia of malignancy model established in mice[3]
Dosage: 32, 64 and 128 mg/kg
Administration: Oral administration (p.o.) or intravenous injection (i.v.), once daily for 7 days
Result: Significantly inhibited the decline of calcium content and protect the bones.
Animal Model: Melanoma A375 cells induced distant bone metastasis model established in mice[3]
Dosage: 100 and 200 mg/kg
Administration: Oral administration (p.o.), once daily for 14 days
Result: Reduced the area of the metastatic lesion significantly to 1.0 mm².
Did not inhibit the metastasis of cancer cells to other organs such as the liver, muscles, and gums.
分子量

410.47

Formula

C22H26N4O4
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

CLIK-148 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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:

CLIK-148215098-90-1CLIK148CLIK 148CathepsinCholecystokinin ReceptorCCK ReceptorCathepsin LCathepsin SCathepsin inhibitorEpoxysuccinateX-ray crystallographyInhibitorinhibitorinhibit

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