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UNC3230

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Chemical Structure| 1031602-63-7 同义名 : -
CAS号 : 1031602-63-7
货号 : A1195872
分子式 : C17H20N4O2S
纯度 : 98%
分子量 : 344.431
MDL号 : MFCD15031190
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(348.4 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 PIPKIγ, a key member of the type I phosphatidylinositol 4-phosphate kinase (PIPKI) family that regulates the spatial-temporal generation of PIP2, has been implicated in diverse biological processes including cell survival, cell polarity, and cell migration[1]. PIPKIγ was frequently upregulated in colorectal cancer and predicted a poor prognosis. Genetic silencing of pan-PIPKIγ suppressed cell proliferation and aerobic glycolysis of colorectal cancer. In contrast, the opposite effects were observed by overexpression of PIPKIγ_i2. Importantly, PIPKIγ-induced prolific effect was largely glycolysis-dependent. Mechanistically, PIPKIγ facilitated activation of PI3K/Akt/mTOR signaling pathways to upregulate c-Myc and HIF1α levels, which regulate expression of glycolytic enzymes to enhance glycolysis. Moreover, pharmacological inhibition by PIPKIγ activity with the specific inhibitor UNC3230 significantly inhibited colorectal cancer glycolysis and tumor growth[2]. UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects. Membrane PIP2 levels are significantly reduced by ~45% in dorsal root ganglia (DRG) neurons treated with 100 nM UNC3230 (~2-fold above the IC50) relative to vehicle controls. UNC3230 significantly reduces lysophosphatidic acid (LPA)-evoked calcium signaling in cultured DRG neurons relative to vehicle. UNC3230 (2 nmol) significantly increases noxious heat-evoked paw withdrawal latency for two hours after intrathecal injection in wild-type mice, indicating an antinociceptive effect. UNC3230 (2 nmol; intrathecal injection) is administered then one hour later co-injected 1 nmol LPA with UNC3230 (2 nmol, intrathecal injection). UNC3230 significantly blunts thermal hyperalgesia and mechanical allodynia compared to vehicle.UNC3230 (2 nmol; intrathecal injection) significantly blunts thermal hyperalgesia and mechanical allodynia in the complete Freund’s adjuvant (CFA)-inflamed hindpaw (relative to vehicle control) but does not affect thermal or mechanical sensitivity in the control (non-inflamed) hindpaw over a multiday time course[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.52mL

2.90mL

1.45mL

29.03mL

5.81mL

2.90mL
参考文献

[1]Wei Ni,et al. SUMOylation is required for PIPK1γ-driven keratinocyte migration and growth. FEBS J. 2019 Dec;286(23):4709-4720.

[2] Wei Peng,et al. Type Iγ phosphatidylinositol phosphate kinase promotes tumor growth by facilitating Warburg effect in colorectal cancer. EBioMedicine. 2019 Jun;44:375-386.

[3]Wright BD, et al. The lipid kinase PIP5K1C regulates pain signaling and sensitization. Neuron. 2014 May 21;82(4):836-47.