UNC3230 | CAS#1031602-63-7 | PIP5K1C inhibitor

MedKoo Cat#: 562948 | Name: UNC3230

Description:

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

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

UNC3230

CAS#1031602-63-7

Theoretical Analysis

MedKoo Cat#: 562948

Name: UNC3230

CAS#: 1031602-63-7

Chemical Formula: C17H20N4O2S

Exact Mass: 344.1307

Molecular Weight: 344.43

Elemental Analysis: C, 59.28; H, 5.85; N, 16.27; O, 9.29; S, 9.31

Price and Availability

Size	Price	Availability
25mg	USD 350.00	2 Weeks
50mg	USD 550.00	2 Weeks
100mg	USD 950.00	2 Weeks
200mg	USD 1,650.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,750.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Related CAS #

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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

View handling instruction

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.

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

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

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.

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.

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