2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. D-I03

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin.

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D-I03 Chemical Structure

D-I03 Chemical Structure

CAS No. : 688342-78-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 96 In-stock
Solution
10 mM * 1 mL in DMSO USD 96 In-stock
Solid
1 mg USD 41 In-stock
5 mg USD 88 In-stock
10 mg USD 160 In-stock
25 mg USD 320 In-stock
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Based on 2 publication(s) in Google Scholar

D-I03 Related Antibodies

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Description

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin[1][2].

IC50 & Target

Ki: 25.8 µM (RAD52)[1][2]
In Vitro

D-I03 (0-10 μM; on days 1 and 3; Capan-1 and UWB1.289 cells) treatment preferentially suppressed the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner[1].
? D-I03 inhibits RAD52 foci formation induced by cisplatin in BCR-ABL1-positive BRCA1-deficient 32Dcl3 murine hematopoietic cell line that expresses GFP-RAD52. In the presence of D-I03 (2.5 μM), the fraction of cells with RAD52 foci is decreased, from 38.7% to 171%; at the same time, the fraction of Cisplatin-treated cells without foci is increased from 48.4% to 71.9%.? D-I03 does not effect on RAD51 foci induced by Cisplatin. Also, D-I03 alone induce neither RAD51 foci nor RAD52 foci (in BRCA1-deficient cells) indicating low genotoxicity of D-I03[1].

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

D-I03 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Capan-1 (BRCA2−) and UWB1.289 (BRCA1+) cells
Concentration: 0 μM, 2.5 μM, 5 μM, or 10 μM
Incubation Time: On days 1 and 3
Result: Preferentially suppressed the growth of Capan-1 and UWB1.289 cells.
In Vivo

D-I03 (50 mg/kg/day; intraperitoneal injection; daily; for 7 days; nu/nu mice) treatment reduces BRCA1-deficient MDA-MB-436 tumor growth. Talazoparib puls D-I03 does not affect the growth of BRCA1-proficient tumors and does not exert any significant toxicity against normal tissues and organs[3].
? Pharmacokinetic and toxicity studies indicates that maximal tolerated dose of D-I03 is ≥50 mg/kg, and t1/2 is 23.4 hours, resulting in >1 μM maximal concentration in peripheral blood[1].

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

Animal Model: Nu/nu mice injected with BRCA1-deficient MDA-MB-436 cells[3]
Dosage: 50 mg/kg/day
Administration: Intraperitoneal injection; daily; for 7 days
Result: Reduced BRCA1-deficient MDA-MB-436 tumor growth.
Molecular Weight

428.64

Formula

C23H36N6S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

S=C(NC1=CC=C2N=C(N3CCN(CC)CC3)C=C(C)C2=C1)NCCN(CC)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (116.65 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 2.3330 mL 11.6648 mL 23.3296 mL
5 mM 0.4666 mL 2.3330 mL 4.6659 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (5.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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: 99.92%

COA (243 KB) HNMR (260 KB) RP-HPLC (206 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3330 mL 11.6648 mL 23.3296 mL 58.3240 mL
5 mM 0.4666 mL 2.3330 mL 4.6659 mL 11.6648 mL
10 mM 0.2333 mL 1.1665 mL 2.3330 mL 5.8324 mL
15 mM 0.1555 mL 0.7777 mL 1.5553 mL 3.8883 mL
20 mM 0.1166 mL 0.5832 mL 1.1665 mL 2.9162 mL
25 mM 0.0933 mL 0.4666 mL 0.9332 mL 2.3330 mL
30 mM 0.0778 mL 0.3888 mL 0.7777 mL 1.9441 mL
40 mM 0.0583 mL 0.2916 mL 0.5832 mL 1.4581 mL
50 mM 0.0467 mL 0.2333 mL 0.4666 mL 1.1665 mL
60 mM 0.0389 mL 0.1944 mL 0.3888 mL 0.9721 mL
80 mM 0.0292 mL 0.1458 mL 0.2916 mL 0.7290 mL
100 mM 0.0233 mL 0.1166 mL 0.2333 mL 0.5832 mL
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D-I03 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:

D-I03688342-78-1DNA/RNA SynthesisssDNArepairRAD52cancersingle-strandannealingD-loopBRCA2-deficientBRCA1-deficienttumorInhibitorinhibitorinhibit

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