2. Apoptosis JAK/STAT Signaling
  3. PKD Pim Apoptosis
  4. CRT0066101 trihydrochloride

CRT0066101 trihydrochloride 是 CRT0066101 (HY-15698) 的三盐酸盐形式。CRT0066101 trihydrochloride 是一种口服有效的 PKD 抑制剂，对 PKD1、PKD2 和 PKD3 的 IC50 值分别为 1 nM、2.5 nM 和 2 nM。CRT0066101 trihydrochloride 也是一种有效的 PIM2 抑制剂，IC50 约为 135.7nM。CRT0066101 trihydrochloride 在 LPS (HY-D1056) 诱发的小鼠肺损伤模型中表现出抗炎活性。CRT0066101 trihydrochloride 具有抗癌作用。

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CRT0066101 trihydrochloride Chemical Structure

CRT0066101 trihydrochloride Chemical Structure

CAS No. : 1781742-22-0

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CRT0066101 trihydrochloride 的其他形式现货产品:

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Other Forms of CRT0066101 trihydrochloride:

CRT0066101 trihydrochloride 相关抗体

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PIM1 PIM2 PIM3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects[1][2][3].

IC50 & Target

PKD1

1 nM (IC50)

PKD3

2 nM (IC50)

PKD2

2.5 nM (IC50)

PIM2

135.7 nM (IC50)

体外研究
(In Vitro)

CRT0066101 trihydrochloride (5 µM; 1 h) 可阻断 Panc-1 和 Panc-28 细胞中基础和 NT 诱导的 pS916-PKD1/2（激活的 PKD1/2）。CRT0066101 消除 NT 诱导的 Hsp27 (pS82-Hsp27) 磷酸化，减弱 PKD1 介导的 NF-κB 激活，并消除 NF-κB 依赖性增殖和促生存蛋白的表达[1] .
CRT0066101 trihydrochloride 显着抑制 Panc-1 细胞增殖，IC50 值为 1 µM。CRT0066101 trihydrochloride 可诱导 Panc-1 细胞凋亡 6-10 倍。CRT0066101 显着降低 Colo357、Panc-1、MiaPaCa-2 和 AsPC-1 细胞的增殖，但对 Capan-2 细胞有一定影响[1]。

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

CRT0066101 trihydrochloride 相关抗体:

Western Blot Analysis[1]

Cell Line: Panc-1 and Panc-28 cells stimulation with neurotensin (NT)
Concentration: 5 µM
Incubation Time: 1 h
Result: Blocked both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2).
体内研究
(In Vivo)

CRT0066101 trihydrochloride (80 mg/kg/天；口服灌胃；每天一次；持续 21 天) 在 Panc-1 原位模型中可有效阻止体内肿瘤生长[1]。 CRT0066101 trihydrochloride (10 mg/kg，腹腔注射，每两天一次共三次) 对 LPS 诱发的 C57BL/6J 小鼠肺炎具有保护作用，并减轻了肺损伤。

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

Animal Model: CR-UK nu/nu mice injected with Panc-1 cells[1]
Dosage: 80 mg/kg/day
Administration: Oral gavage; once daily; for 21 days
Result: Potently blocked tumor growth in vivo.
Animal Model: LPS (HY-D1056)-induced lung injury in C57BL/6J mice[3]
Dosage: 10 mg/kg
Administration: i.p., once every two days for 3 times
Result: Inhibited the expression of MyD88 and TLR4, inhibited the phosphorylation of NF-κB, ERK and JNK.
分子量

447.79

Formula

C18H25Cl3N6O
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

CRT0066101 trihydrochloride 相关分类

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  • 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:

CRT0066101 trihydrochloride1781742-22-0PKDPimApoptosisProtein kinase DPim kinasesPKD1PKD2PKD3PIM2anticancer effectspS82-Hsp27C57BL/6J mouseanti-inflammatoryInhibitorinhibitorinhibit

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目录号：
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