2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. I-138

I-138 is an orally active, reversible inhibitor of USP1-UAF1 (IC50: 4.1 nM; Ki: 5.4 nM), structurally related to ML323 (HY-17543). I-138 induces monoubiquitination of FANCD2 and PCNA in cells and eliminates USP1 autocleavage in cells.

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I-138 Chemical Structure

I-138 Chemical Structure

CAS No. : 2098211-50-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 542 In-stock
Solution
10 mM * 1 mL in DMSO USD 542 In-stock
Solid
1 mg USD 250 In-stock
5 mg USD 470 In-stock
10 mg USD 760 In-stock
25 mg USD 1430 In-stock
50 mg USD 2600 In-stock
100 mg USD 4200 In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

I-138 Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

View All Isoforms
USP1 USP2 USP7 USP8 USP30 UCHL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

I-138 is an orally active, reversible inhibitor of USP1-UAF1 (IC50: 4.1 nM; Ki: 5.4 nM), structurally related to ML323 (HY-17543). I-138 induces monoubiquitination of FANCD2 and PCNA in cells and eliminates USP1 autocleavage in cells[1].

In Vitro

I-138 (0.5 μM; 4 h) eliminates USP1 self-lysis in HAP-1 USP1 WT and knockout cells[1].
I-138 (0.5 μM; 4 h) induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells[1].
(0.01-10 μM; 10 days) dose-dependently inhibits MDA-MB-436 cells viability and don't affect HCC1954 cells[1].

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

I-138 Related Antibodies
In Vivo

I-138 (50 mg/kg/day; po, for 41 days) results USP1 inhibition and modest antitumor activity in mice bearing MDA-MB-436 tumors. However, the combination of I-138 and Niraparib (HY-10619), a PARP inhibitor, benefit the BRCA1/2 mutant tumors inhibition in vivo[1].

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

492.50

Formula

C26H23F3N6O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1NC2=CN=C(C3=CC=CC=C3C(C)C)N=C2N1CC4=CC=C(C5=NC(C(F)(F)F)=CN5C)C=C4
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 : 100 mg/mL (203.05 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 2.0305 mL 10.1523 mL 20.3046 mL
5 mM 0.4061 mL 2.0305 mL 4.0609 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
×
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: 2.5 mg/mL (5.08 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: 2.5 mg/mL (5.08 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. 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 (25.0 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)

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

Purity: 99.88%

SDS (251 KB)

COA (249 KB) HNMR (137 KB) RP-HPLC (245 KB)

Handling Instructions (2659 KB)
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 1 mM 2.0305 mL 10.1523 mL 20.3046 mL 50.7614 mL
5 mM 0.4061 mL 2.0305 mL 4.0609 mL 10.1523 mL
10 mM 0.2030 mL 1.0152 mL 2.0305 mL 5.0761 mL
15 mM 0.1354 mL 0.6768 mL 1.3536 mL 3.3841 mL
20 mM 0.1015 mL 0.5076 mL 1.0152 mL 2.5381 mL
25 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0305 mL
30 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6920 mL
40 mM 0.0508 mL 0.2538 mL 0.5076 mL 1.2690 mL
50 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
60 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8460 mL
80 mM 0.0254 mL 0.1269 mL 0.2538 mL 0.6345 mL
100 mM 0.0203 mL 0.1015 mL 0.2030 mL 0.5076 mL
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I-138 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:

I-1382098211-50-6I138I 138DeubiquitinaseDUBsInhibitorinhibitorinhibit

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