SETDB1-TTD-IN-1 TFA
Based on 6 publication(s) in Google Scholar
SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD.
For research use only. We do not sell to patients.
- Purity: 99.77%
- Formula: C30H32F3N5O4
- Molecular Weight:583.60
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Publications Citing Use of MedChemExpress (MCE) SETDB1-TTD-IN-1 TFA
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
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SETDB1/KMT2G |
SETDB1-TTD-IN-1 (compound (R,R)-59) TFA shows some activity for 53BP1 and JMJD2A, with Kds of 4.3 μM and 86 μM, respectively. SETDB1-TTD-IN-1 TFA does not show activity against 14 of the 16 tested tudor domains (Kd>100 μM)[1].
SETDB1-TTD-IN-1 (2.5-40 μM) TFA efficiently and dose-dependently stabilizes the SETDB1-TTD protein in HEK293T cells[1].
SETDB1-TTD-IN-1 (2.5-40 μM; 24 h) TFA significantly affected the expression of 72 genes in human acute monocytic leukemia THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 583.60
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Formula C30H32F3N5O4
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Color White to off-white
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SMILES
CN1C[C@@H](C2=CC=C(OCC3=CC=CC=C3)C=C2)C[C@@H](NC4=NC5=C(C(N4CC=C)=O)NC=C5)C1.OC(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (6)
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Journal Impact Factor
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Most Recent
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Autophagy
SETDB1 enhances starvation-induced lipophagy by inhibiting m6A-mediated mRNA decay via DDX5 methylation. [Abstract]2026 May 17:1-23. PMID: 42087801 -
Cell Death Dis
SETDB1 is critically required for uveal melanoma growth and represents a promising therapeutic target. [Abstract]2025 Oct 24;16(1):754. PMID: 41136387 -
BMC Biol
SETDB1 targeting SESN2 regulates mitochondrial damage and oxidative stress in renal ischemia-reperfusion injury. [Abstract]2024 Oct 23;22(1):246. PMID: 39443993 -
J Inflamm Res
Mechanisms of Acetate in Alleviating SETDB1-Linked Neuroinflammation and Cognitive Impairment in a Mouse Model of OSA. [Abstract]2025 May 7:18:5931-5950. PMID: 40357375 -
Mol Cell Endocrinol
Estrogen increases Setdb1 cytoplasmic localization to stabilize Serpinh1 and improve protein homeostasis in osteoblasts. [Abstract]2025 May 3:112568. PMID: 40324678 -
Exp Hematol
CBX7 inhibitors affect H3K9 methyltransferase-regulated gene repression in leukemic cells. [Abstract]2024 Nov 27:104691. PMID: 39613290
Solvent & Solubility
DMSO : 100 mg/mL (171.35 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
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: ≥ 5 mg/mL (8.57 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.57 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.
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 (protect from light, stored under nitrogen)
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 (275 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]. Guo Y, et, al. Structure-Guided Discovery of a Potent and Selective Cell-Active Inhibitor of SETDB1 Tudor Domain. Angew Chem Int Ed Engl. 2021 Apr 12;60(16):8760-8765. [Content Brief]
[2]. Uguen M, et, al. SETDB1 Triple Tudor Domain Ligand, (R, R)-59, Promotes Methylation of Akt1 in Cells. ACS Chem Biol. 2023 Aug 18;18(8):1846-1853. [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 (protect from light, stored under nitrogen). 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 | 1.7135 mL | 8.5675 mL | 17.1350 mL | 42.8376 mL |
| 5 mM | 0.3427 mL | 1.7135 mL | 3.4270 mL | 8.5675 mL | |
| 10 mM | 0.1714 mL | 0.8568 mL | 1.7135 mL | 4.2838 mL | |
| 15 mM | 0.1142 mL | 0.5712 mL | 1.1423 mL | 2.8558 mL | |
| 20 mM | 0.0857 mL | 0.4284 mL | 0.8568 mL | 2.1419 mL | |
| 25 mM | 0.0685 mL | 0.3427 mL | 0.6854 mL | 1.7135 mL | |
| 30 mM | 0.0571 mL | 0.2856 mL | 0.5712 mL | 1.4279 mL | |
| 40 mM | 0.0428 mL | 0.2142 mL | 0.4284 mL | 1.0709 mL | |
| 50 mM | 0.0343 mL | 0.1714 mL | 0.3427 mL | 0.8568 mL | |
| 60 mM | 0.0286 mL | 0.1428 mL | 0.2856 mL | 0.7140 mL | |
| 80 mM | 0.0214 mL | 0.1071 mL | 0.2142 mL | 0.5355 mL | |
| 100 mM | 0.0171 mL | 0.0857 mL | 0.1714 mL | 0.4284 mL |
SETDB1-TTD-IN-1 TFA Related Classifications
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