2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. TMP195

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.

For research use only. We do not sell to patients.

CAS No. : 1314891-22-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 17 publication(s) in Google Scholar

TMP195 Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    View All HDAC Isoform Specific Products:

    View All Isoforms
    HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    IC50 & Target[1]

    HDAC9

    9 nM (IC50)

    HDAC7

    46 nM (IC50)

    HDAC5

    106 nM (IC50)

    HDAC4

    111 nM (IC50)

    HDAC8

    11700 nM (IC50)

    HDAC6

    47800 nM (IC50)

    In Vitro

    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.

    TMP195 Related Antibodies
    In Vivo

    TMP195 treatment alters the tumour microenvironment and reduces tumour burden and pulmonary metastases by modulating macrophage phenotypes. TMP195 induces the recruitment and differentiation of highly phagocytic and stimulatory macrophages within tumors. Combining TMP195 with chemotherapy regimens or T-cell checkpoint blockade in this model significantly enhances the durability of tumour reduction[2].

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

    456.42

    Formula

    C23H19F3N4O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NCC(C)(C)C1=COC(C2=CC=CC=C2)=N1)C3=CC(C4=NOC(C(F)(F)F)=N4)=CC=C3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1910 mL 10.9548 mL 21.9096 mL
    5 mM 0.4382 mL 2.1910 mL 4.3819 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, 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 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.
    • Protocol 2

      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.

    • Protocol 1

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 8.33 mg/mL (18.25 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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

    Purity: 99.82%

    SDS (393 KB)

    COA (246 KB) LCMS (106 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 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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    TMP195 Related Classifications

    Help & FAQs
    • 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:

    TMP1951314891-22-9TMP 195TMP-195HDACHistone deacetylasesInhibitorinhibitorinhibit

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