Ac-Lys(CoA)-NH2 TFA
Based on 1 publication(s) in Google Scholar
Ac-Lys(CoA)-NH2 TFA (Ac-Lys(coenzyme A)-NH2 TFA) is a selective p300 histone acetyltransferase (HAT) inhibitor with an IC50 of approximately 50 nM or 500 nM.
For research use only. We do not sell to patients.
- Purity : 98.52%
- CAS No.: 3112948-91-8
- Formula: C33H54F3N10O21P3S
- Molecular Weight:1108.82
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ac-Lys(CoA)-NH2 TFA
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Biological Activity
Description
IC50 & Target
[1]|
p300 ~50-500 nM (IC50) |
In Vitro
Ac-Lys(CoA)-NH2 (1 min) TFA is a potent and selective p300 inhibitor with an IC50 of 0.5 µM, while its inhibitory effect on PCAF is much weaker, with an IC50 of 200 µM[2].
Ac-Lys(CoA)-NH2 (0-120 pmol per oocyte; 12 h) TFA selectively inhibits p300-activated transcription in Xenopus oocytes with an IC50 of approximately 30 pmol/cell, while exerting only a minimal effect on PCAF-mediated activation[2].
Ac-Lys(CoA)-NH2 TFA TFA is a potent p300/CBP HAT inhibitor with Ki = 19 nM in biochemical assays[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3112948-91-8
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Appearance Solid
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Molecular Weight 1108.82
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Formula C33H54F3N10O21P3S
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Color White to off-white
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SMILES
O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(OP(OCC(C)(C)[C@@H](O)C(NCCC(NCCSCC(NCCCC[C@@H](C(N)=O)NC(C)=O)=O)=O)=O)(O)=O)(O)=O)O[C@H]1N2C=NC3=C(N)N=CN=C32.O=C(O)C(F)(F)F
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Synonyms
Ac-Lys(coenzyme A)-NH2 TFA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Rep
DOCK1 inhibitor Box5 (TFA) suppresses proliferation of AML cell lines and prolongs survival in AML xenograft models. [Abstract]2026 May 11;16(1):21377. PMID: 42108312
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (90.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.25 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.25 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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 (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Cebrat M, et al. Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorganic & medicinal chemistry. 2003 Jul 31;11(15):3307-13. [Content Brief]
[2]. Lau OD, et al. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Molecular cell. 2000 Mar;5(3):589-95. [Content Brief]
[3]. Cole PA, et al. Chemical probes for histone-modifying enzymes. Nature chemical biology. 2008 Oct;4(10):590-7. [Content Brief]
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 (sealed storage, away from moisture). 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 | 0.9019 mL | 4.5093 mL | 9.0186 mL | 22.5465 mL |
| 5 mM | 0.1804 mL | 0.9019 mL | 1.8037 mL | 4.5093 mL | |
| 10 mM | 0.0902 mL | 0.4509 mL | 0.9019 mL | 2.2546 mL | |
| 15 mM | 0.0601 mL | 0.3006 mL | 0.6012 mL | 1.5031 mL | |
| 20 mM | 0.0451 mL | 0.2255 mL | 0.4509 mL | 1.1273 mL | |
| 25 mM | 0.0361 mL | 0.1804 mL | 0.3607 mL | 0.9019 mL | |
| 30 mM | 0.0301 mL | 0.1503 mL | 0.3006 mL | 0.7515 mL | |
| 40 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.5637 mL | |
| 50 mM | 0.0180 mL | 0.0902 mL | 0.1804 mL | 0.4509 mL | |
| 60 mM | 0.0150 mL | 0.0752 mL | 0.1503 mL | 0.3758 mL | |
| 80 mM | 0.0113 mL | 0.0564 mL | 0.1127 mL | 0.2818 mL |
Ac-Lys(CoA)-NH2 TFA Related Classifications
HY-131035 Related Classifications
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Keywords
- Ac-Lys(CoA)-NH2
- 3112948-91-8
- Ac-Lys(coenzyme A)-NH2
- Histone Acetyltransferase
- HATs
- HAT
- C. elegans development
- HAT inhibitor
- PCAF
- acetyl transfer
- bisubstrate analog
- chromatin-template transcription
- muscle cell differentiation
- p300/CBP histone acetyltransferase
- p73 acetylation
- transcriptional activation
- Inhibitor
- inhibitor
- inhibit