UNC3230
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 562948

CAS#: 1031602-63-7

Description: UNC3230 is a selective inhibitor of lipid kinase PIP5K1C. It acts by lowering PIP2 levels in DRG neurons and attenuating hypersensitivity. UNC3230 lowered PIP2 levels in DRG neurons and attenuated hypersensitivity when administered intrathecally or into the hindpaw. PIP5K1C regulates PIP2-dependent nociceptive signaling and suggest that PIP5K1C is a therapeutic target for chronic pain.

Chemical Structure

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UNC3230
CAS# 1031602-63-7
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 562948
Name: UNC3230
CAS#: 1031602-63-7
Chemical Formula: C17H20N4O2S
Exact Mass: 344.13
Molecular Weight: 344.430
Elemental Analysis: C, 59.28; H, 5.85; N, 16.27; O, 9.29; S, 9.31

Price and Availability

Size Price Availability Quantity
25mg USD 350 2 Weeks
50mg USD 550 2 Weeks
100mg USD 950 2 Weeks
200mg USD 1650 2 Weeks
500mg USD 2650 2 Weeks
1g USD 3750 2 Weeks
2g USD 6450 2 Weeks
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Synonym: UNC3230; UNC-3230; UNC 3230;

IUPAC/Chemical Name: 5-(Cyclohexanecarboxamido)-2-(phenylamino)thiazole-4-carboxamide

InChi Key: RZCNASHHHSKTGP-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H20N4O2S/c18-14(22)13-16(21-15(23)11-7-3-1-4-8-11)24-17(20-13)19-12-9-5-2-6-10-12/h2,5-6,9-11H,1,3-4,7-8H2,(H2,18,22)(H,19,20)(H,21,23)

SMILES Code: O=C(C1=C(NC(C2CCCCC2)=O)SC(NC3=CC=CC=C3)=N1)N

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
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Biological target: UNC3230 is a selective inhibitor of lipid kinase PIP5K1C.
In vitro activity: Furthermore, inhibition of PIPKIγ activity with the chemical inhibitor UNC3230 suppresses fibronectin secretion in a dose-dependent manner, whereas depletion of Cdk5 enhances fibronectin secretion. With total internal reflection fluorescence microscopy, it was found that secreted fibronectin appears as round dots, which colocalize with Tks5 and CD9 but not with Zyxin. These data suggest that Cdk5-mediated PIPKIγ90 phosphorylation regulates cell invasion by controlling PIPKIγ90 activity and fibronectin secretion.-Li, L., Kołodziej, T., Jafari, N., Chen, J., Zhu, H., Rajfur, Z., Huang, C. Cdk5-mediated phosphorylation regulates phosphatidylinositol 4-phosphate 5-kinase type I γ 90 activity and cell invasion. Reference: Li L, Kołodziej T, Jafari N, Chen J, Zhu H, Rajfur Z, Huang C. Cdk5-mediated phosphorylation regulates phosphatidylinositol 4-phosphate 5-kinase type I γ 90 activity and cell invasion. FASEB J. 2019 Jan;33(1):631-642. doi: 10.1096/fj.201800296R. Epub 2018 Jul 24. PMID: 30040488; PMCID: PMC6355064.
In vivo activity: Here, phosphatidylinositol 4-phosphate 5 kinase type 1C (PIP5K1C) was found to be expressed at higher levels than any other PIP5K and, based on experiments with Pip5k1c(+/-) mice, generates at least half of all PIP2 in DRG neurons. Additionally, Pip5k1c haploinsufficiency reduces pronociceptive receptor signaling and TRPV1 sensitization in DRG neurons as well as thermal and mechanical hypersensitivity in mouse models of chronic pain. A small molecule inhibitor of PIP5K1C (UNC3230) was identified in a high-throughput screen. UNC3230 lowered PIP2 levels in DRG neurons and attenuated hypersensitivity when administered intrathecally or into the hindpaw. Our studies reveal that PIP5K1C regulates PIP2-dependent nociceptive signaling and suggest that PIP5K1C is a therapeutic target for chronic pain. Reference: Wright BD, Loo L, Street SE, Ma A, Taylor-Blake B, Stashko MA, Jin J, Janzen WP, Frye SV, Zylka MJ. The lipid kinase PIP5K1C regulates pain signaling and sensitization. Neuron. 2014 May 21;82(4):836-47. doi: 10.1016/j.neuron.2014.04.006. PMID: 24853942; PMCID: PMC4074510.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.0 87.10
DMF 30.0 87.10
Ethanol 0.2 0.58

Preparing Stock Solutions

The following data is based on the product molecular weight 344.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: Li L, Kołodziej T, Jafari N, Chen J, Zhu H, Rajfur Z, Huang C. Cdk5-mediated phosphorylation regulates phosphatidylinositol 4-phosphate 5-kinase type I γ 90 activity and cell invasion. FASEB J. 2019 Jan;33(1):631-642. doi: 10.1096/fj.201800296R. Epub 2018 Jul 24. PMID: 30040488; PMCID: PMC6355064.
In vitro protocol: Li L, Kołodziej T, Jafari N, Chen J, Zhu H, Rajfur Z, Huang C. Cdk5-mediated phosphorylation regulates phosphatidylinositol 4-phosphate 5-kinase type I γ 90 activity and cell invasion. FASEB J. 2019 Jan;33(1):631-642. doi: 10.1096/fj.201800296R. Epub 2018 Jul 24. PMID: 30040488; PMCID: PMC6355064.
In vivo protocol: Wright BD, Loo L, Street SE, Ma A, Taylor-Blake B, Stashko MA, Jin J, Janzen WP, Frye SV, Zylka MJ. The lipid kinase PIP5K1C regulates pain signaling and sensitization. Neuron. 2014 May 21;82(4):836-47. doi: 10.1016/j.neuron.2014.04.006. PMID: 24853942; PMCID: PMC4074510.

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1: Wright BD, Simpson C, Stashko M, Kireev D, Hull-Ryde EA, Zylka MJ, Janzen WP. Development of a High-Throughput Screening Assay to Identify Inhibitors of the Lipid Kinase PIP5K1C. J Biomol Screen. 2015 Jun;20(5):655-62. doi: 10.1177/1087057114564057. Epub 2014 Dec 22. PubMed PMID: 25534829; PubMed Central PMCID: PMC4610143.

2: Wright BD, Loo L, Street SE, Ma A, Taylor-Blake B, Stashko MA, Jin J, Janzen WP, Frye SV, Zylka MJ. The lipid kinase PIP5K1C regulates pain signaling and sensitization. Neuron. 2014 May 21;82(4):836-47. doi: 10.1016/j.neuron.2014.04.006. PubMed PMID: 24853942; PubMed Central PMCID: PMC4074510.