| Bioactivity | 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[1]. | ||||||||||||
| Target | IC50: ~41 nM (Phosphatidylinositol 4-phosphate 5 kinase type 1C (PIP5K1C)) | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| In Vivo | 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[1]. 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[1]. 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[1]. | ||||||||||||
| Name | UNC3230 | ||||||||||||
| CAS | 1031602-63-7 | ||||||||||||
| Formula | C17H20N4O2S | ||||||||||||
| Molar Mass | 344.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Wright BD, et al. The lipid kinase PIP5K1C regulates pain signaling and sensitization. Neuron. 2014 May 21;82(4):836-47. [2]. Peng W, 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. Development of a High-Throughput Screening Assay to Identify Inhibitors of the Lipid Kinase PIP5K1C. J Biomol Screen. 2015 Jun;20(5):655-62. |
UNC3230
CAS: 1031602-63-7 F: C17H20N4O2S W: 344.43
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K
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