TMP195
Based on 17 publication(s) in Google Scholar
TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.82%
- No. CAS: 1314891-22-9
- Fòrmula: C23H19F3N4O3
- Peso molecular:456.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) TMP195
More- Cancer Cell. 2021 Oct 11;39(10):1361-1374.e9. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Adv Sci (Weinh). 2025 Mar 31:e2501553. [Abstract]
- Nucleic Acids Res. 2022 Mar 21;50(5):2566-2586. [Abstract]
- J Neuroinflammation. 2025 Nov 26;22(1):280. [Abstract]
- Cell Death Dis. 2023 Feb 13;14(2):117. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- EMBO J. 2024 Nov;43(21):4954-4983. [Abstract]
- ACS Appl Mater Interfaces. 2023 Mar 1;15(8):10371-10382. [Abstract]
- J Med Chem. 2024 Sep 12;67(17):15098-15117. [Abstract]
- Commun Biol. 2024 Oct 4;7(1):1257. [Abstract]
- Commun Biol. 2021 Jul 15;4(1):878. [Abstract]
- Clin Epigenetics. 2022 Nov 12;14(1):147. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Virology. 2024 Nov 15:601:110305. [Abstract]
- SSRN. 2023 Jul 17.
- Research Square Preprint. 2022 Feb.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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IHC
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Flow Cytometry
Actividad biológica
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HDAC9 9 nM (IC50) |
HDAC7 46 nM (IC50) |
HDAC5 106 nM (IC50) |
HDAC4 111 nM (IC50) |
HDAC8 11700 nM (IC50) |
HDAC6 47800 nM (IC50) |
TMP195 blocks the accumulation of CCL2 protein in the supernatants of monocyte-derived macrophage differentiation cultures. TMP195 significantly increases the amount of CCL1 protein secreted by the monocytes compared to vehicle group. In the transcriptional profiling data from the PHA-stimulated PBMC experiments, CCL2 and CCL1 are respectively down- or upregulated by TMP195[1]. TMP195 occupies the acetyllysine-binding site of class IIa HDACs. TMP195 competes against binding of HDAC7 to a variety of side-chain modifications on the same peptide backbone, despite no interference with the activity of other acetyllysine reader proteins BRD4 (IC50>50 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1314891-22-9
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Appearance Solid
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Peso molecular 456.42
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Fòrmula C23H19F3N4O3
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Color White to off-white
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SMILES
O=C(NCC(C)(C)C1=COC(C2=CC=CC=C2)=N1)C3=CC(C4=NOC(C(F)(F)F)=N4)=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2021 Oct 11;39(10):1361-1374.e9. PMID: 34478639 -
Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Adv Sci (Weinh)
HDAC6 and USP9X Control Glutamine Metabolism by Stabilizing GS to Promote Glioblastoma Tumorigenesis. [Abstract]2025 Mar 31:e2501553. PMID: 40162736 -
Nucleic Acids Res
Transcriptomic and genomic studies classify NKL54 as a histone deacetylase inhibitor with indirect influence on MEF2-dependent transcription. [Abstract]2022 Mar 21;50(5):2566-2586. PMID: 35150567 -
J Neuroinflammation
FOXA2 regulated by HDAC3-mediated deacetylation attenuates neuropathic pain by modulating microglial lipid metabolism and synaptic pruning dysregulation. [Abstract]2025 Nov 26;22(1):280. PMID: 41299504 -
Cell Death Dis
Dynamic differentiation of F4/80+ tumor-associated macrophage and its role in tumor vascularization in a syngeneic mouse model of colorectal liver metastasis. [Abstract]2023 Feb 13;14(2):117. PMID: 36781833
TMP195 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 13;14(2):117. [Abstract]
The liver and CRLM samples at 14 dpi with/out TMP195 (50 mg/kg, i.p.) treatment.
TMP195 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 13;14(2):117. [Abstract]
IHC with anti-CD34 antibodies showed greatly disturbed neovascularization within CRLM in TMP195 (50 mg/kg, i.p.)-treated liver biopsies.
TMP195 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 13;14(2):117. [Abstract]
Flow cytometry analysis on 14 dpi liver biopsies of the tumor area and liver area with/without TMP195 (50 mg/kg, i.p.) treatment. TMP195 treatment greatly reduced the number of CD11bint F4/80+ cells whereas increased that of CD11b+ F4/80− cells in the tumors.
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
EMBO J
Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]2024 Nov;43(21):4954-4983. PMID: 39294473 -
ACS Appl Mater Interfaces
Engineered Apoptosis-Bioinspired Nanoparticles Initiate Immune Cascade for Cancer Immunotherapy of Malignant Ascites. [Abstract]2023 Mar 1;15(8):10371-10382. PMID: 36786554 -
J Med Chem
Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death. [Abstract]2024 Sep 12;67(17):15098-15117. PMID: 39145486 -
Commun Biol
Selective inhibition of HDAC class IIA as therapeutic intervention for KMT2A-rearranged acute lymphoblastic leukemia. [Abstract]2024 Oct 4;7(1):1257. PMID: 39362994
TMP195 purchased from MedChemExpress. Usage Cited in: Commun Biol. 2024 Oct 4;7(1):1257. [Abstract]
Dose response curves for TMP195 in several KMT2A-rearranged ALL cell line models using 4-day MTT assay.
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Commun Biol
Three-dimensional CRISPR screening reveals epigenetic interaction with anti-angiogenic therapy. [Abstract]2021 Jul 15;4(1):878. PMID: 34267311 -
Clin Epigenetics
Repression of the PRELP gene is relieved by histone deacetylase inhibitors through acetylation of histone H2B lysine 5 in bladder cancer. [Abstract]2022 Nov 12;14(1):147. PMID: 36371227 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Virology
H1N1 swine influenza viruses upregulate NEU1 expression through histone H3 acetylation regulated by HDAC2. [Abstract]2024 Nov 15:601:110305. PMID: 39566266 -
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Solvente y solubilidad
DMSO : 100 mg/mL (219.10 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, 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.
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.
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: ≥ 3 mg/mL (6.57 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: 3 mg/mL (6.57 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 15% Cremophor EL 85% Saline
Solubility: 8.33 mg/mL (18.25 mM); Suspended solution; Need ultrasonic
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.
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.
Protocolo
Recombinant HDAC7 catalytic domain (amino acids 483-903) is labeled with DyLight 650 and applied to an arrayed library of 3,868 immobilized 20-mer peptides. Arrays are conducted using an automated TECAN HS4 microarray processing station, initiated by incubation with blocking buffer for 30 min at 30°C followed by ishing with saline containing 50 mM Tris Base and 0.1% Tween-20 (pH 7.2) before incubation with the labeled HDAC7 protein for 120 min at 4°C. In the case of TMP195 competition experiments, the labeled protein is pre-incubated with TMP195 for 30 min before application to the array. The microarrays are then ished before being dried and imaged with an scanner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: For all mouse experiments, mice are treated with intraperitoneal (i.p.) injections of 50 μL of the vehicle dimethyl sulfoxide (DMSO) or 50 μL of TMP195 dissolved in 100% DMSO at a final concentration of 50 mg per kg daily[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lobera M, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat Chem Biol. 2013 May;9(5):319-25. [Content Brief]
[2]. Guerriero JL, et al. Class IIa HDAC inhibition reduces breast tumors and metastases through anti-tumor macrophages. Nature. 2017 Mar 16;543(7645):428-432. [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, 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 | 2.1910 mL | 10.9548 mL | 21.9096 mL | 54.7741 mL |
| 5 mM | 0.4382 mL | 2.1910 mL | 4.3819 mL | 10.9548 mL | |
| 10 mM | 0.2191 mL | 1.0955 mL | 2.1910 mL | 5.4774 mL | |
| 15 mM | 0.1461 mL | 0.7303 mL | 1.4606 mL | 3.6516 mL | |
| 20 mM | 0.1095 mL | 0.5477 mL | 1.0955 mL | 2.7387 mL | |
| 25 mM | 0.0876 mL | 0.4382 mL | 0.8764 mL | 2.1910 mL | |
| 30 mM | 0.0730 mL | 0.3652 mL | 0.7303 mL | 1.8258 mL | |
| 40 mM | 0.0548 mL | 0.2739 mL | 0.5477 mL | 1.3694 mL | |
| 50 mM | 0.0438 mL | 0.2191 mL | 0.4382 mL | 1.0955 mL | |
| 60 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.9129 mL | |
| 80 mM | 0.0274 mL | 0.1369 mL | 0.2739 mL | 0.6847 mL | |
| 100 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.5477 mL |
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