2. Cell Cycle/DNA Damage Apoptosis Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. Deubiquitinase Apoptosis Bcr-Abl STAT c-Myc
  4. CT1113

CT1113 is a selective, orally active USP25/USP28 inhibitor. CT1113 inhibits cancer cell proliferation, induces apoptosis, and causes G2/S phase cell cycle arrest. CT1113 reduces the levels of total BCR-ABL1, phosphorylated BCR-ABL1, total STAT5, and phosphorylated STAT5, but does not alter the mRNA level of BCR-ABL1. CT1113 is applicable to research related to pancreatic cancer, colon cancer, and acute leukemia.

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CT1113

CT1113 Chemical Structure

CAS No. : 2523435-18-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

CT1113 Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

View All Isoforms
USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15

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Abl Bcr-Abl

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

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Description

CT1113 is a selective, orally active USP25/USP28 inhibitor. CT1113 inhibits cancer cell proliferation, induces apoptosis, and causes G2/S phase cell cycle arrest. CT1113 reduces the levels of total BCR-ABL1, phosphorylated BCR-ABL1, total STAT5, and phosphorylated STAT5, but does not alter the mRNA level of BCR-ABL1. CT1113 is applicable to research related to pancreatic cancer, colon cancer, and acute leukemia[1][2].

IC50 & Target[1]

STAT5

 

BCR-ABL1

 

In Vitro

CT1113 (500 nM; 1-24 h) reduces c-MYC levels in various cancer cell lines within 1-2 h, decreases USP25, USP28, LSD1 and Tankyrase levels after 24 h, and enhances the ubiquitination of c-MYC and Tankyrase, without affecting the stability of p53 or CHK2[1].
CT1113 potently inhibits the proliferation of various tumor cell lines, with an EC50 of 65 nM in control HCT116 cells; its antiproliferative effect is largely targeted, as co-overexpression of USP25 and USP28 reduces the sensitivity of cells to CT1113[1].
CT1113 (0-600 nM; 72 h) potently inhibits the growth of human Ph+ALL cell lines, Ba/F3 cells expressing mutant BCR-ABL1, and primary Ph+ALL cells in vitro, with an IC50 of approximately 200 nM[2].
CT1113 (0-600 nM; 72 h) significantly induces apoptosis in human Ph+ALL cell lines, Ba/F3 cells expressing mutant BCR-ABL1, and primary Ph+ALL cells[2].
CT1113 (0-600 nM; 72 h) inhibits the phosphorylation of BCR-ABL1 and STAT5, and reduces the total protein levels of BCR-ABL1 and STAT5 in human Ph+ALL cell lines (this effect can be blocked by proteasome inhibition)[2].
CT1113 (0-600 nM; 72 h) enhances the ubiquitination level of BCR-ABL1, thereby promoting its proteasomal degradation in human Ph+ALL cell lines[2].
CT1113 (0-600 nM; 72 h) does not alter BCR-ABL1 mRNA levels in human Ph+ALL cell lines[2].

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

CT1113 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116, HGC27, SMMC7721, diverse cancer cell lines
Concentration: 500 nM
Incubation Time: 24 h
Result: Dramatically reduced c-MYC levels within 1-2 h across diverse cancer cell lines.\n
Dramatically decreased levels of USP25, USP28, LSD1, and Tankyrase after 24 h of treatment with 500 nM.\n
Increased ubiquitination of c-MYC and Tankyrase proteins.\nShowed no significant destabilization of p53 or CHK2 proteins.
In Vivo

CT1113 exhibits strong anti-tumor activity in a mouse pancreatic cancer xenograft model, significantly suppressing tumor growth, reducing c-MYC levels, and decreasing tumor cell proliferation[1].
CT1113 exhibits strong anti-tumor activity in a mouse colon cancer CDX model, significantly suppressing tumor growth[1].
CT1113(21 days) treatment of healthy C57BL/6 mice causes reversible mild body weight loss but no overt toxicity, does not disrupt intestinal crypt proliferation despite reducing overall intestinal c-MYC levels, and does not impair testicular tissue structure or spermatogonia proliferation[1].

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

463.60

Formula

C25H29N5O2S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CNC1=C(C(N[C@@H]2CC3=CC=C(N4CC5NC(CC5)C4)C=C3OC2)=O)SC6=NC(C)=CC=C16
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 (215.70 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 2.1570 mL 10.7852 mL 21.5703 mL
5 mM 0.4314 mL 2.1570 mL 4.3141 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
×
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: ≥ 5 mg/mL (10.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (10.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 1 mM 2.1570 mL 10.7852 mL 21.5703 mL 53.9258 mL
5 mM 0.4314 mL 2.1570 mL 4.3141 mL 10.7852 mL
10 mM 0.2157 mL 1.0785 mL 2.1570 mL 5.3926 mL
15 mM 0.1438 mL 0.7190 mL 1.4380 mL 3.5951 mL
20 mM 0.1079 mL 0.5393 mL 1.0785 mL 2.6963 mL
25 mM 0.0863 mL 0.4314 mL 0.8628 mL 2.1570 mL
30 mM 0.0719 mL 0.3595 mL 0.7190 mL 1.7975 mL
40 mM 0.0539 mL 0.2696 mL 0.5393 mL 1.3481 mL
50 mM 0.0431 mL 0.2157 mL 0.4314 mL 1.0785 mL
60 mM 0.0360 mL 0.1798 mL 0.3595 mL 0.8988 mL
80 mM 0.0270 mL 0.1348 mL 0.2696 mL 0.6741 mL
100 mM 0.0216 mL 0.1079 mL 0.2157 mL 0.5393 mL
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CT1113 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:

CT11132523435-18-7CT 1113CT-1113DeubiquitinaseApoptosisBcr-AblSTATc-MycDUBsMycTNKSBCR-ABL1leukemia cellsc-MYCUSP28LSD1STAT5apoptosisG2/S cell cycle arrestUSP25Inhibitorinhibitorinhibit

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