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
* <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. 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].

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.

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：

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
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
Identification of Required Host Factors for SARS-CoV-2 Infection in Human Cells [ Cell, 2020, S0092-8674(20)31394-5] PubMed: 33147445
HDAC7 is an actionable driver of therapeutic antibody resistance by macrophages from CLL patients [ Oncogene, 2020, 10.1038/s41388-020-01394-w] PubMed: 32709923

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。