2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. OTUB2-IN-1

OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) .

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

OTUB2-IN-1 Chemical Structure

OTUB2-IN-1 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

OTUB2-IN-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) [1].

In Vitro

OTUB2-IN-1 (0-40 μM) reduces PD-L1 levels in tumor cells (NCI-H358, SK-MES-1, and NCI-H226) in a dose-dependent manner, but it is unable to affect OTUB2 stability[1].
OTUB2-IN-1 (0-50 μM; 1 h) does not interfere with protein interactions between OTUB2 and PD-L1[1].
OTUB2-IN-1 (10 μM; 0-4 d) can’t inhibit the viability of B16-F10 tumor cells[1].

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

OTUB2-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: B16-F10 tumor cells
Concentration: 10 μM
Incubation Time: 0-4 d
Result: OTUB2-IN-1 did not show significant inhibitory effects on the viability of B16-F10 tumor cells over a period of up to four days.

Western Blot Analysis[1]

Cell Line: NCI-H358，SK-MES-1, NCI-H226
Concentration: 0-40 μM
Incubation Time:
Result: Reduced PD-L1 levels in a dose-dependent manner across these cell lines, indicating effective inhibition of OTUB2's functional activity regarding PD-L1 stabilization.
However, it did not affect the stability of OTUB2 itself, suggesting that the inhibitor specifically disrupts the PD-L1 regulatory function of OTUB2 without altering OTUB2 protein stability.
In Vivo

OTUB2-IN-1 (20 mg/kg; i.p.; daily for five days) suggests the potential to enhance immune recognition and immune response of tumor cells in mice implanted with B16-F10 cells[1].
OTUB2-IN-1 （20 mg/kg; i.p.; daily for five days）reduces the expression of YAP and phosphorylated p65 in mice implanted with LL/2 cells; reduces phosphorylated Akt expression in mice implanted with B16-F10 cells and it reduces phosphorylated p65 expression in mice implanted with KLN205 cells[1].

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

Animal Model: C57BL/6 mice implanted with B16-F10 cells or LL/2 cells [1]
Dosage: 20 mg/kg; daily for five days
Administration: i.p
Result: Reduced the expression of PD-L1 on tumor cells, suggesting its potential in enhancing immune recognition and response against tumor cells.
Did not significantly impact tumor cell viability directly, indicating its action might be more about modulating immune evasion mechanisms rather than cytotoxic effects.
Increased the infiltration of cytotoxic T cells within the tumors, suggesting that reducing PD-L1 levels can indeed make the tumor more susceptible to immune attack.within the tumors, suggesting that reducing PD-L1 levels can indeed make the tumor more susceptible to immune attack.
Molecular Weight

434.49

Formula

C19H18N2O6S2
Appearance

Solid

Color

Orange to red

SMILES

OC(CCCCCN1C(S/C(C1=O)=C2C(C=CC=C3)=C3N(CC(O)=O)C\2=O)=S)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (115.08 mM; Need ultrasonic; 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 2.3015 mL 11.5077 mL 23.0155 mL
5 mM 0.4603 mL 2.3015 mL 4.6031 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 (protect from light). 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
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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

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Volume (start)

V1

=
Concentration (final)

C2

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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    90% Corn Oil

    Solubility: 5 mg/mL (11.51 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 20 mg/mL (46.03 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  15% Cremophor EL    85% Saline

    Solubility: 10 mg/mL (23.02 mM); Suspended solution; Need ultrasonic

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 1 mM 2.3015 mL 11.5077 mL 23.0155 mL 57.5387 mL
5 mM 0.4603 mL 2.3015 mL 4.6031 mL 11.5077 mL
10 mM 0.2302 mL 1.1508 mL 2.3015 mL 5.7539 mL
15 mM 0.1534 mL 0.7672 mL 1.5344 mL 3.8359 mL
20 mM 0.1151 mL 0.5754 mL 1.1508 mL 2.8769 mL
25 mM 0.0921 mL 0.4603 mL 0.9206 mL 2.3015 mL
30 mM 0.0767 mL 0.3836 mL 0.7672 mL 1.9180 mL
40 mM 0.0575 mL 0.2877 mL 0.5754 mL 1.4385 mL
50 mM 0.0460 mL 0.2302 mL 0.4603 mL 1.1508 mL
60 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9590 mL
80 mM 0.0288 mL 0.1438 mL 0.2877 mL 0.7192 mL
100 mM 0.0230 mL 0.1151 mL 0.2302 mL 0.5754 mL
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OTUB2-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:

OTUB2-IN-1DeubiquitinaseDUBsPD-L1CTLtumors C57BL/6 miceInhibitorinhibitorinhibit

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