2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. UNC9512

UNC9512 is a selective 53BP1 inhibitor with an IC50 of 0.46 μM, and a Kd values of 0.17 μM. UNC9512 binds 53BP1 and its tandem Tudor domain, disrupts histone H4 interaction, and inhibits 53BP1 activity. UNC9512 can be used as a probe for DNA damage repair and Gene editing.

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UNC9512

UNC9512 Chemical Structure

CAS No. : 3032393-24-8

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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

UNC9512 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE UNC9512

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Description

UNC9512 is a selective 53BP1 inhibitor with an IC50 of 0.46 μM, and a Kd values of 0.17 μM. UNC9512 binds 53BP1 and its tandem Tudor domain, disrupts histone H4 interaction, and inhibits 53BP1 activity. UNC9512 can be used as a probe for DNA damage repair and Gene editing[1][2].

In Vitro

UNC9512 binds to modified 53BP1 (mutated to match zebrafish 53BP1 key amino acids) with a Kd of approximately 3 μM[1].
UNC9512 (up to 100 μM; 1 h) is highly selective for the 53BP1 tandem Tudor domain, with no measurable binding to SETDB1 TTD, UHRF1 TTD, PHF19 Tudor-PHD, KDM7B JmjC-PHD, CBX2 CD, CDYL2 CD, or MPP8 CD at concentrations up to 100 μM[2].
UNC9512 (0-200 μM; overnight) shows minimal toxicity to HEK293T, U2OS[2].
UNC9512 (0-100 μM; 1 h pre-incubation + 2 h post-IR incubation) dose-dependently reduces 53BP1-dependent foci formation in ionizing radiation-treated U2OS cells, achieving a ~3-fold reduction at 50 μM[2].

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

UNC9512 Related Antibodies
In Vivo

UNC9512 (60 μM; microinjection; single dose at 1-cell stage) produces a shift in pigmentation rescue phenotypes in Casper zebrafish with mitfaI113Q mutations[1].
UNC9512 (60 μM; microinjection; single dose at 1-cell stage) increase mean Ki rate of CRISPR editing of kcnh6a in TL/Ekk zebrafish[1].
UNC9512 (60 μM; microinjection; single dose at 1-cell stage) increase mean Ki rate and maintains 100% Ki efficiency of CRISPR editing of sox10 in TL/Ekk zebrafish[1].
UNC9512 (60 μM; microinjection; single dose at 4-8 cell stage) produces reductions in background indels, NHEJ, and MMEJ for CRISPR editing of sox10 in TL/Ekk zebrafish[1].

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

Animal Model: Casper zebrafish[1]
Dosage: 60 μM
Administration: microinjection; single dose at 1-cell stage
Result: Increased the mean near WT pigmentation KI rate 1.62-fold.
Produced a significant difference in proportions of larvae across pigmentation rescue groups compared to SS6 alone.
Resulted in 14% KI rate and 4.3% near WT pigmentation KI rate.
Animal Model: TL/Ekk zebrafish[1]
Dosage: 60 μM
Administration: microinjection; single dose at 1-cell stage
Result: Increased the mean KI rate 1.54-fold (from 1.71% with SS2 alone to 2.63%), though this was not statistically significant.
Produced a non-significant trend towards a higher mean KI-score, lower mean background indels, and higher mean PGE/indel ratio.
Identified 7 PGE positive larvae among 484 injected embryos.
Caused a non-significant reduction in the median percentage of NHEJ-associated indels (≤4 bp) targeting kcnh6a.\nIncreased the mean KI rate 1.19-fold (from 84.33% with SS3 alone to 93.75%), with 100% KI across all experiments.
Produced non-significant changes in mean KI-score (11.82 vs 14.45 for SS3 alone), mean background indels, and mean PGE/indel ratio.
Identified 15 PGE positive larvae among 18 sampled larvae.
Caused a non-significant reduction in the median percentage of NHEJ-associated indels (≤4 bp) targeting sox10.
Animal Model: TL/Ekk zebrafish[1]
Dosage: 60 μM
Administration: microinjection; single dose at 4-8 cell stage
Result: Resulted in no significant change in KI rate compared to SS3 alone at the 1-cell stage, with a mean KI rate of 83.33%.
Produced a non-significant reduction in mean background indels, a non-significant reduction in mean NHEJ-associated indels, and a non-significant reduction in mean MMEJ-associated indels.
Achieved a mean KI-score of 11.25 and mean PGE/indel ratio of 0.28.
Molecular Weight

538.64

Formula

C31H34N6O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(C2=CC=C(C3=C2)CNC3=O)=CC=C1)[C@H]4CCCN(C4)C(C5=NC=CC(N6CCN(CC6)C)=C5)=O
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 (185.65 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 1.8565 mL 9.2826 mL 18.5653 mL
5 mM 0.3713 mL 1.8565 mL 3.7131 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.

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  • Dilution Calculator

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

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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 (4.64 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 (4.64 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 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 1.8565 mL 9.2826 mL 18.5653 mL 46.4132 mL
5 mM 0.3713 mL 1.8565 mL 3.7131 mL 9.2826 mL
10 mM 0.1857 mL 0.9283 mL 1.8565 mL 4.6413 mL
15 mM 0.1238 mL 0.6188 mL 1.2377 mL 3.0942 mL
20 mM 0.0928 mL 0.4641 mL 0.9283 mL 2.3207 mL
25 mM 0.0743 mL 0.3713 mL 0.7426 mL 1.8565 mL
30 mM 0.0619 mL 0.3094 mL 0.6188 mL 1.5471 mL
40 mM 0.0464 mL 0.2321 mL 0.4641 mL 1.1603 mL
50 mM 0.0371 mL 0.1857 mL 0.3713 mL 0.9283 mL
60 mM 0.0309 mL 0.1547 mL 0.3094 mL 0.7736 mL
80 mM 0.0232 mL 0.1160 mL 0.2321 mL 0.5802 mL
100 mM 0.0186 mL 0.0928 mL 0.1857 mL 0.4641 mL
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UNC9512 Related Classifications

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  • 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:

UNC95123032393-24-8UNC 9512UNC-9512DNA/RNA Synthesisionizing radiationcolorectal cancerbreast cancer53BP1human 53BP1 tandem Tudor domainnon-homologous end joiningzebrafish 53BP1glioblastomanonsmall cell lung cancerhistone H4Inhibitorinhibitorinhibit

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