TMP195

Catalog No.S8502 Batch:S850202

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Technical Data

Formula

C23H19F3N4O3
Molecular Weight 456.42 CAS No. 1314891-22-9
Solubility (25°C)* In vitro DMSO 91 mg/mL (199.37 mM)
Ethanol 91 mg/mL (199.37 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with Ki of 59, 60, 26 and 15nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
Targets
HDAC9 [1]
(Cell-free assay)		 HDAC7 [1]
(Cell-free assay)		 HDAC4 [1]
(Cell-free assay)		 HDAC5 [1]
(Cell-free assay)
15 nM(Ki) 26 nM(Ki) 59 nM(Ki) 60 nM(Ki)
In vitro

TMP195 has low potency in recombinant class I and IIb HDAC assays, enabling full inhibition of class IIa HDAC activity without inhibition of other HDACs. TMP195 blocks the accumulation of CCL2 protein in the supernatants of monocyte-derived macrophage differentiation cultures and significantly increases the amount of CCL1 protein secreted by the monocytes compared to vehicle (DMSO)-treated M-CSF plus GM-CSF cultures[1]. TMP195 influences human monocyte responses to the colony-stimulating factors CSF-1 and CSF-2 in vitro[2].
In vivo

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 tumours. TMP195 treatment significantly decreases proliferating tumour cells, most notably at the leading edge of the tumour. The anti-tumour macrophage phenotype induced by TMP195 treatment thus enhances the efficacy and durability of both standard chemotherapeutic regimens and checkpoint blockade immunotherapy in this mouse model of breast cancer[2].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Human monocytes

  • Concentrations

    300 nM

  • Incubation Time

    5 days

  • Method

    Monocytes were differentiated into antigen presenting cells in RPMI Medium 1640 supplemented with GlutaMAX fetal bovine serum (10% v/v), IL-4 (10 ng/ml), GM-CSF (50 ng/ml), penicillin (100 U/ml), and streptomycin (100 μg/ml) for 5 days in the presence of either 0.1% (v/v) DMSO or 300 nM TMP195. Cells were collected by washing and incubation with a solution of 5 mM EDTA in PBS (Ca2+/Mg2+-free), before flow cytometric analysis.
Animal Study:

[2]
  • Animal Models

    MMTV-PyMT transgenic mice

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Selleck's TMP195 has been cited by 20 publications

Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5] PubMed: 38823394
Histone 4 lysine 5/12 acetylation enables developmental plasticity of Pristionchus mouth form [ Nat Commun, 2023, 14(1):2095] PubMed: 37055396
Histone 4 lysine 5/12 acetylation enables developmental plasticity of Pristionchus mouth form [ Nat Commun, 2023, 14(1):2095] PubMed: 37055396
HDAC9-mediated epithelial cell cycle arrest in G2/M contributes to kidney fibrosis in male mice [ Nat Commun, 2023, 14(1):3007] PubMed: 37230975
PATJ inhibits histone deacetylase 7 to control tight junction formation and cell polarity [ Cell Mol Life Sci, 2023, 80(11):333] PubMed: 37878054
PATJ inhibits histone deacetylase 7 to control tight junction formation and cell polarity [ Cell Mol Life Sci, 2023, 80(11):333] PubMed: 37878054
Reprogramming Short-Chain Fatty Acid Metabolism Mitigates Tissue Damage for Streptococcus pyogenes Necrotizing Skin Infection [ Res Sq, 2023, rs.3.rs-3689163] PubMed: 38196634
TMP195 Exerts Antitumor Effects on Colorectal Cancer by Promoting M1 Macrophages Polarization [ Int J Biol Sci, 2022, 18(15):5653-5666] PubMed: 36263186
HDAC7 Activates IKK/NF-κB Signaling to Regulate Astrocyte-Mediated Inflammation [ Mol Neurobiol, 2022, 1-17] PubMed: 35871708
Epigenetic targeting of the ACE2 and NRP1 viral receptors limits SARS-CoV-2 infectivity [ Clin Epigenetics, 2021, 13(1):187] PubMed: 34635175

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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