2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. UBA5-IN-1

UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5.

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UBA5-IN-1 Chemical Structure

UBA5-IN-1 Chemical Structure

CAS No. : 1831169-11-9

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5 mg USD 700 In-stock
10 mg USD 1120 In-stock
25 mg USD 2250 In-stock
50 mg USD 3650 In-stock
100 mg USD 5900 In-stock
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Based on 1 publication(s) in Google Scholar

UBA5-IN-1 Related Antibodies

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  • Purity & Documentation

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Description

UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5[1].

IC50 & Target

IC50: 4.0 μM (UBA5), 78.5 μM (UAE), 66.8 μM (NAE)[1]
In Vitro

UBA5-IN-1 (0.1-1000 μM) shows dose-dependent inhibition effect to UBA5 with an IC50 value of 4.0 μM, and inhibits UAE and NAE with IC50 values of 78.5 and 66.8 μM, respectively[1].
UBA5-IN-1 (0-5 μM) inhibits UBA5 non-competitively with respect to ATP[1].
UBA5-IN-1 (10 μM) shows no effect on ATP binding to human kinase[1].
UBA5-IN-1 (0-50 μM; 72 h) effects cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5[1].

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

UBA5-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Sk-Luci6 cancer cells with high expression levels of UBA5
Concentration: 0-50 μM
Incubation Time: 0-72 h
Result: Showed selective anti-proliferative activity for Sk-Luci6 cancer cells which expressed higher UBA5 protein levels, but showed no anti-proliferative activity to MRC9 lung fibroblasts and A549 carcinoma cells.
Molecular Weight

912.16

Formula

C26H40F6N10O11S2Zn
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C(F)(F)F)([O-])=O.O=S(C(F)(F)F)([O-])=O.NC1=C(N=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](C(NCCCCCC([N]45[Zn+2]67[N@@](CC[N]6([H])CC[N@]7([H])CC5)([H])CC4)=O)=O)O3)C2=NC=N1
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: 

DMF : 100 mg/mL (109.63 mM; Need ultrasonic)

DMSO : 50 mg/mL (54.81 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 1.0963 mL 5.4815 mL 10.9630 mL
5 mM 0.2193 mL 1.0963 mL 2.1926 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)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (1.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (1.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / DMF 1 mM 1.0963 mL 5.4815 mL 10.9630 mL 27.4075 mL
5 mM 0.2193 mL 1.0963 mL 2.1926 mL 5.4815 mL
10 mM 0.1096 mL 0.5481 mL 1.0963 mL 2.7407 mL
15 mM 0.0731 mL 0.3654 mL 0.7309 mL 1.8272 mL
20 mM 0.0548 mL 0.2741 mL 0.5481 mL 1.3704 mL
25 mM 0.0439 mL 0.2193 mL 0.4385 mL 1.0963 mL
30 mM 0.0365 mL 0.1827 mL 0.3654 mL 0.9136 mL
40 mM 0.0274 mL 0.1370 mL 0.2741 mL 0.6852 mL
50 mM 0.0219 mL 0.1096 mL 0.2193 mL 0.5481 mL
DMF 60 mM 0.0183 mL 0.0914 mL 0.1827 mL 0.4568 mL
80 mM 0.0137 mL 0.0685 mL 0.1370 mL 0.3426 mL
100 mM 0.0110 mL 0.0548 mL 0.1096 mL 0.2741 mL
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UBA5-IN-1 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:

UBA5-IN-11831169-11-9E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseSk-Luci6UAENAEATPhuman kinaseMRC9A549Inhibitorinhibitorinhibit

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