TMP195

Catalog No.S8502 Synonyms: TFMO 2

For research use only.

TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.

TMP195 Chemical Structure

CAS No. 1314891-22-9

Selleck's TMP195 has been cited by 12 Publications

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Biological Activity

Description TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
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 Research:

[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 Research:

[2]

  • Animal Models: MMTV-PyMT transgenic mice
  • Dosages: 50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 456.42
Formula

C23H19F3N4O3

CAS No. 1314891-22-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(CNC(=O)C1=CC=CC(=C1)C2=NOC(=N2)C(F)(F)F)C3=COC(=N3)C4=CC=CC=C4

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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