TMP195

製品コードS8502 バッチS850201

印刷

化学情報

Chemical Structure Synonyms TFMO 2 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H19F3N4O3
分子量 456.42 CAS No. 1314891-22-9
Solubility (25°C)* 体外 DMSO 91 mg/mL (199.37 mM)
Ethanol 91 mg/mL (199.37 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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. This compound 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]. It 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. This compound induces the recruitment and differentiation of highly phagocytic and stimulatory macrophages within tumours. Its treatment significantly decreases proliferating tumour cells, most notably at the leading edge of the tumour. The anti-tumour macrophage phenotype induced by this chemical thus enhances the efficacy and durability of both standard chemotherapeutic regimens and checkpoint blockade immunotherapy in this mouse model of breast cancer[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human monocytes
濃度 300 nM
反応時間 5 days
実験の流れ

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.
動物実験 動物モデル MMTV-PyMT transgenic mice
投薬量 50 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/23524983/
  • https://pubmed.ncbi.nlm.nih.gov/28273064/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Reprogramming aerobic metabolism mitigates Streptococcus pyogenes tissue damage in a mouse necrotizing skin infection model [ Nat Commun, 2025, 16(1):2559] PubMed: 40089471
Low butyrate concentrations exert anti-inflammatory and high concentrations exert pro-inflammatory effects on macrophages [ J Nutr Biochem, 2025, 144:109962] PubMed: 40381959
The microbial metabolite butyrate enhances the effector and memory functions of murine CD8+ T cells and improves anti-tumor activity [ Front Med (Lausanne), 2025, 12:1577906] PubMed: 40630475
Sorbate induces lysine sorbylation through noncanonical activities of class I HDACs to regulate the expression of inflammation genes [ Sci Adv, 2025, 11(22):eadv1071] PubMed: 40446041
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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