UCK2 Inhibitor-3

Cat. No.: HY-148396 Purity: 98.65%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC₅₀ value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC₅₀s of 56 μM and 16 μM.

For research use only. We do not sell to patients.

UCK2 Inhibitor-3 Chemical Structure

CAS No. : 2376687-49-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

DNA Polymerase

In Vitro

Dihydroorotate dehydrogenase (DHODH), a rate-limiting enzyme in mammalian de novo pyrimidine synthesis. UCK2 can make up for DHODH in a certain extent, in infected or rapidly dividing cells for uridine salvage. DHODH inhibition has antiviral and anticancer significance, while UCK2 Inhibitor-3 suppress nucleoside salvage in cells both in the presence and absence of DHODH inhibitors^[1].
UCK2 Inhibitor-3 (compound 135416439) is an inhibitor against pyrimidine salvage enzyme, non-competitive with Uridine and ATP with K_i values of 13 μM and 12 μM, respectively^[1].
UCK2 Inhibitor-3 (50 μM) inhibits UCK2 with inhibition rate of 31.3%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

474.31

Formula

C₁₉H₁₃BrFN₅O₂S

CAS No.

2376687-49-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(Br)C=C1)CSC(N=C2C3=CNN2C4=CC=C(F)C=C4)=NC3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (105.42 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1083 mL	10.5416 mL	21.0833 mL
5 mM	0.4217 mL	2.1083 mL	4.2167 mL
10 mM	0.2108 mL	1.0542 mL	2.1083 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (10.54 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.65%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (250 KB) HNMR (136 KB) RP-HPLC (239 KB) LCMS (109 KB)

Handling Instructions (2659 KB)

References

[1]. Okesli-Armlovich A, et al. Discovery of small molecule inhibitors of human uridine-cytidine kinase 2 by high-throughput screening. Bioorg Med Chem Lett. 2019 Sep 15;29(18):2559-2564. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1083 mL	10.5416 mL	21.0833 mL	52.7081 mL
	5 mM	0.4217 mL	2.1083 mL	4.2167 mL	10.5416 mL
	10 mM	0.2108 mL	1.0542 mL	2.1083 mL	5.2708 mL
	15 mM	0.1406 mL	0.7028 mL	1.4056 mL	3.5139 mL
	20 mM	0.1054 mL	0.5271 mL	1.0542 mL	2.6354 mL
	25 mM	0.0843 mL	0.4217 mL	0.8433 mL	2.1083 mL
	30 mM	0.0703 mL	0.3514 mL	0.7028 mL	1.7569 mL
	40 mM	0.0527 mL	0.2635 mL	0.5271 mL	1.3177 mL
	50 mM	0.0422 mL	0.2108 mL	0.4217 mL	1.0542 mL
	60 mM	0.0351 mL	0.1757 mL	0.3514 mL	0.8785 mL
	80 mM	0.0264 mL	0.1318 mL	0.2635 mL	0.6589 mL
	100 mM	0.0211 mL	0.1054 mL	0.2108 mL	0.5271 mL

UCK2 Inhibitor-3 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UCK2 Inhibitor-32376687-49-7DNA/RNA Synthesisdihydroorotate dehydrogenaseantiviralanticancerrapidly dividing cellsuridine salvageInhibitorinhibitorinhibit

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