THZ-P1-2
目录号 : GC39823
THZ-P1-2 是一种有效的PI5P4K激酶抑制剂，对PI5P4Kα和PI5P4Kβ的IC50值分别为0.95μM和5.9μM。
Cas No.:2058075-45-7
Sample solution is provided at 25 µL, 10mM.
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THZ-P1-2 is a potent inhibitor of PI5P4K kinase, with the IC50 values of 0.95μM and 5.9μM for PI5P4Kα and PI5P4Kβ, respectively [1]. THZ-P1-2 binds in the active site and covalently modifies cysteine residues of the PI5P4K kinases[2]. THZ-P1-2 has been widely used in cell models to regulate autophagy[3].
In vitro, THZ-P1-2 treatment for 4 hours inhibited SARS-CoV-2 replication in Calu-3 cells with an EC50 value of 0.2µM and inhibited cell viability (CC50=16µM)[4]. THZ-P1-2 treatment (6.4µM) for 48h significantly inhibited NB4 cell viability and enhanced venetoclax-induced apoptosis[5]. Treatment with 6.4µM THZ-P1-2 for 72h significantly reduced Jurkat cell viability and induced DNA damage, triggered apoptosis, and disrupted mitochondrial homeostasis and autophagic flux in cells[6].
References:
[1] Manz T D, Sivakumaren S C, Yasgar A, et al. Structure–activity relationship study of covalent pan-phosphatidylinositol 5-phosphate 4-kinase inhibitors[J]. ACS medicinal chemistry letters, 2019, 11(3): 346-352.
[2] Sivakumaren S C, Shim H, Zhang T, et al. Targeting the PI5P4K lipid kinase family in cancer using covalent inhibitors[J]. Cell chemical biology, 2020, 27(5): 525-537. e6.
[3] Lima K, Nogueira F L, Cipelli M, et al. Potency and efficacy of pharmacological PIP4K2 inhibitors in acute lymphoblastic leukemia[J]. European Journal of Pharmacology, 2024, 977: 176723.
[4] Karim M, Mishra M, Lo C W, et al. PIP4K2C inhibition reverses autophagic flux impairment induced by SARS-CoV-2[J]. Nature Communications, 2025, 16(1): 6397.
[5] Lima K, Carvalho M F L, Pereira-Martins D A, et al. Pharmacological inhibition of PIP4K2 potentiates venetoclax-induced apoptosis in acute myeloid leukemia[J]. International Journal of Molecular Sciences, 2023, 24(23): 16899.
[6] Lima K, Pereira-Martins D A, de Miranda L B L, et al. The PIP4K2 inhibitor THZ-P1-2 exhibits antileukemia activity by disruption of mitochondrial homeostasis and autophagy[J]. Blood cancer journal, 2022, 12(11): 151.
THZ-P1-2 是一种有效的PI5P4K激酶抑制剂，对PI5P4Kα和PI5P4Kβ的IC50值分别为0.95μM和5.9μM[1]。THZ-P1-2通过结合于PI5P4K激酶的活性位点，共价修饰半胱氨酸残基[2]。THZ-P1-2已在细胞模型中广泛应用于调控自噬过程[3]。
在体外，使用THZ-P1-2处理Calu-3细胞4小时可抑制SARS-CoV-2病毒复制，EC50值为0.2µM，同时对细胞活力产生抑制（CC50=16µM）[4]。以6.4µM的THZ-P1-2处理NB4细胞48小时能显著抑制细胞活力，并增强Venetoclax诱导的细胞凋亡[5]。使用6.4µM的THZ-P1-2处理Jurkat细胞72小时可显著降低细胞活力，诱导DNA损伤，触发细胞凋亡，并破坏线粒体稳态及自噬通量[6]。
| Cell experiment [1]: | |
Cell lines | NB4 cells |
Preparation Method | A total of 2×104 NB4 cells/well were seeded into the appropriate medium in 96-well plates and incubated for 48 hours with various concentrations of THZ-P1-2 (1.6, 3.2, and 6.4µM). Next, 10μl of methyl thiazolyl tetrazolium (MTT) solution (5mg/mL) was added and incubated at 37°C and 5% CO2 for 4 hours. The reaction was terminated with 100μl of anhydrous isopropanol solution of 0.1M HCl. Cell viability was assessed by measuring the absorbance at 570nm. |
Reaction Conditions | 1.6, 3.2, and 6.4µM; 48h |
Applications | THZ-P1-2 treatment inhibited the cell viability of NB4 cells in a dose-dependent manner. |
References: | |
| Cas No. | 2058075-45-7 | SDF | |
| Canonical SMILES | O=C(C(C=C1)=CC=C1NC(/C=C/CN(C)C)=O)NC2=CC=CC(NC3=CC(C4=CNC5=CC=CC=C45)=NC=N3)=C2 | ||
| 分子式 | C31H29N7O2 | 分子量 | 531.61 |
| 溶解度 | Soluble in DMSO | 储存条件 | 4°C, protect from light |
| 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 | 1.8811 mL | 9.4054 mL | 18.8108 mL |
| 5 mM | 376.2 μL | 1.8811 mL | 3.7622 mL |
| 10 mM | 188.1 μL | 940.5 μL | 1.8811 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet