Home Epigenetics HDAC inhibitor TMP195 For research use only.

TMP195

Synonyms: TFMO 2

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.

TMP195 Chemical Structure

TMP195 Chemical Structure

CAS No. 1314891-22-9

Purity & Quality Control

TMP195 Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models MMTV-PyMT transgenic mice
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 456.42 Formula

C23H19F3N4O3
CAS No. 1314891-22-9 SDF Download TMP195 SDF
Smiles CC(C)(CNC(=O)C1=CC=CC(=C1)C2=NOC(=N2)C(F)(F)F)C3=COC(=N3)C4=CC=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (199.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble


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In vivo
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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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