IACS-9571
Based on 2 publication(s) in Google Scholar
IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
For research use only. We do not sell to patients.
- CAS No.: 1800477-30-8
- Formula: C32H42N4O8S
- Molecular Weight:642.76
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) IACS-9571
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Biological Activity
Description
IC50 & Target
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
10.82 μM
Compound: IACS-9571
|
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by Cell Titer-Glo assay
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[PMID: 35385803] |
| HeLa | EC50 |
0.05 μM
Compound: 8i; IACS-9571
|
Inhibition of Flag-tagged TRIM24-PHD/bromodomain (unknown origin) expressed in human HeLa cells for 2 hrs by AlphaLisa assay
Inhibition of Flag-tagged TRIM24-PHD/bromodomain (unknown origin) expressed in human HeLa cells for 2 hrs by AlphaLisa assay
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[PMID: 26061247] |
| LNCaP | IC50 |
12.15 μM
Compound: IACS-9571
|
Antiproliferative activity against human LNCaP cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human LNCaP cells measured after 96 hrs by Cell Titer-Glo assay
|
[PMID: 35385803] |
| LNCaP C4-2B | IC50 |
13.63 μM
Compound: IACS-9571
|
Antiproliferative activity against human LNCaP C4-2B cells measured after 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against human LNCaP C4-2B cells measured after 96 hrs by Cell Titer-Glo assay
|
[PMID: 35385803] |
In Vitro
IACS-9571 shows excellent cellular potency with EC50 of 50 nM. IACS-9571 (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 is a selective dual TRIM24/BRPF1 inhibitor (Kd = 1.3/2.1 nM) with 9- and 21-fold selectivity against BRPF2 and BRPF3, respectively. IACS-9571 does not interact with the BET sub-family of bromodomains, displaying greater than 7,700-fold selectivity versus BRD4(1, 2) relative to TRIM24[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1800477-30-8
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Molecular Weight 642.76
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Formula C32H42N4O8S
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SMILES
O=S(C1=CC=C(OC)C(OC)=C1)(NC2=C(OC3=CC(OCCC)=CC(OCCCCN(C)C)=C3)C=C(N4C)C(N(C)C4=O)=C2)=O
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Synonyms
ASIS-P040
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
2025 Aug 19;122(33):e2507571122. PMID: 40815626 -
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (155.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (3.89 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 (3.89 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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-
-
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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.
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
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5558 mL | 7.7790 mL | 15.5579 mL | 38.8948 mL |
| 5 mM | 0.3112 mL | 1.5558 mL | 3.1116 mL | 7.7790 mL | |
| 10 mM | 0.1556 mL | 0.7779 mL | 1.5558 mL | 3.8895 mL | |
| 15 mM | 0.1037 mL | 0.5186 mL | 1.0372 mL | 2.5930 mL | |
| 20 mM | 0.0778 mL | 0.3889 mL | 0.7779 mL | 1.9447 mL | |
| 25 mM | 0.0622 mL | 0.3112 mL | 0.6223 mL | 1.5558 mL | |
| 30 mM | 0.0519 mL | 0.2593 mL | 0.5186 mL | 1.2965 mL | |
| 40 mM | 0.0389 mL | 0.1945 mL | 0.3889 mL | 0.9724 mL | |
| 50 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.7779 mL | |
| 60 mM | 0.0259 mL | 0.1296 mL | 0.2593 mL | 0.6482 mL | |
| 80 mM | 0.0194 mL | 0.0972 mL | 0.1945 mL | 0.4862 mL | |
| 100 mM | 0.0156 mL | 0.0778 mL | 0.1556 mL | 0.3889 mL |