IHMT-MST1-58
目录号 : GC69261IHMT-MST1-58 是一种有效的、选择性的 STE20-like protein 1 kinase (MST1) 抑制剂，具有口服活性，IC50 值为 23 nM。IHMT-MST1-58 可用于 1 型或 2 型糖尿病的研究。
Cas No.:2414484-25-4
Sample solution is provided at 25 µL, 10mM.
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IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes[1].
IHMT-MST1-58 (compound 19) shows good activity against MST1 with an IC50 value of 23 nM[1].
IHMT-MST1-58 (1 μM) displays strong inhibitory activity against MST1 (IC50 = 23 nM), weak activity against MST2 (IC50 = 652 nM), but no activity against NEK3 even at 10 μM (IC50 > 10 μM) [1].
IHMT-MST1-58 (1 μM) shows strong binding affinity to MST1 and weak binding affinity to MST2 with Kd values of 240 nM and 2.7 μM[1].
IHMT-MST1-58 (0.1-10 μM; 1-2 h) inhibits the phosphorylation of MST1 in vitro[1].
IHMT-MST1-58 (0.03, 0.1 and 0.3 μM; 48 h) exhibits a significant protective effect of β cells from the damage caused by inflammatory cytokines[1].
Western Blot Analysis[1]
| Cell Line: | HepG2 liver cells, RAW264.7, RPE1 and HL7702 cells; INS-1 and RIN-m5F cell lines |
| Concentration: | 0-10 μM |
| Incubation Time: | 2 h (HepG2 liver cells, RAW264.7, RPE1, and HL7702 cells) |
| Result: | Inhibited the H2O2-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation in a dose-dependent manner in all four cell lines. Inhibited the phosphorylation of LATS1 (T1079) and YAP (S127) in HepG2 cells. Showed strong inhibition of MST1 phosphorylation and its downstream MOB1 autophosphorylation in a dose-dependent manner in both cell lines. |
IHMT-MST1-58 (compound 19) (p.o, 50 mg/kg/day, QD) combination with metformin led to the decline of fasting blood glucose, show protective effect of β cells and decrease the hemoglobin A1c level in the STZ-induced T1D/T2D mouse models[1].
Pharmacokinetic Parameters of IHMT-MST1-58 in different species (i.v. or p.o; 1 mg/kg, 5 mg/kg and 10 mg/kg)[1].
| mice | rats | beagle dogs | ||||
| parameter | i.v.(1 mg/kg) | p.o.(10 mg/kg) | i.v.(1 mg/kg) | p.o.(10 mg/kg) | i.v.(1 mg/kg) | p.o.(10 mg/kg) |
| AUC0-t(ng/mL*h) | 501.1 | 5583 | 2553±155.1 | 4858±2648 | 764.5±82.9 | 4939±1067 |
| t1/2(h) | 1.7 | 1.81 | 3.51±0.34 | 3.03±0.2 | 6.47±0.71 | 5.79±1.09 |
| Cmax/F (ng/mL) | 1240 | 1922 | 944.0±219.1 | 1717±276 | 466.7±45.2 | 1113±417 |
| F(%) | - | 110.8 | - | 73.3±40.1 | - | 106.5±20.9 |
| Animal Model: | mice[1] | ||||||||||||
| Dosage: | 50 mg/kg | ||||||||||||
| Administration: | oral, single | ||||||||||||
| Result: |
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| Animal Model: | T1D mouse models and T2D mouse models[1] |
| Dosage: | 50 mg/kg |
| Administration: | p.o, 50 mg/kg/day, QD |
| Result: | Decreased the FBG level, improved the food intake and water consumption, had low HbA1c and a good antidiabetic effect, improved the histological structure of the islet. |
| Animal Model: | mice, Sprague Dawley rats, and beagle dogs[1] |
| Dosage: | 1 mg/kg, 5 mg/kg and 10 mg/kg |
| Administration: | intravenous injection and oral administration |
| Result: | Displayed acceptable pharmacokinetic properties in different species. |
[1]. Yun Wu, et al. Discovery of IHMT-MST1-58 as a Novel, Potent, and Selective MST1 Inhibitor for the Treatment of Type 1/2 Diabetes. J Med Chem. 2022 Sep 8;65(17):11818-11839
| Cas No. | 2414484-25-4 | SDF | Download SDF |
| 分子式 | C21H22N6O3S | 分子量 | 438.5 |
| 溶解度 | DMSO : 100 mg/mL (228.05 mM; ultrasonic and warming and heat to 80°C) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2805 mL | 11.4025 mL | 22.805 mL |
| 5 mM | 0.4561 mL | 2.2805 mL | 4.561 mL |
| 10 mM | 0.2281 mL | 1.1403 mL | 2.2805 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet