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TMP195

Cat. No. M6176
TMP195 Structure
Synonym:

TFMO 2

Size Price Availability Quantity
5mg USD 115  USD115 In stock
10mg USD 200  USD200 In stock
25mg USD 420  USD420 In stock
50mg USD 700  USD700 In stock
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Quality Control & Documentation
Biological Activity

In vitro: TMP195 blocks the accumulation of CCL2 protein in the supernatants of monocyte-derived macrophage differentiation cultures. TMP195 significantly increases the amount of CCL1 protein secreted by the monocytes compared to vehicle group. In the transcriptional profiling data from the PHA-stimulated PBMC experiments, CCL2 and CCL1 are respectively down- or upregulated by TMP195. TMP195 occupies the acetyllysine-binding site of class IIa HDACs. TMP195 competes against binding of HDAC7 to a variety of side-chain modifications on the same peptide backbone, despite no interference with the activity of other acetyllysine reader proteins BRD4 (IC50>50 μM).

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 tumors. Combining TMP195 with chemotherapy regimens or T-cell checkpoint blockade in this model significantly enhances the durability of tumour reduction.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Mouse
Formulation DMSO
Dosages 50 mg/kg
Administration i.p.
Chemical Information
Molecular Weight 456.42
Formula C23H19F3N4O3
CAS Number 1314891-22-9
Solubility (25°C) 82 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Cassetta L, et al. Cell Res. Repolarizing macrophages improves breast cancer therapy.

[2] Guerriero JL, et al. Nature. Class IIa HDAC inhibition reduces breast tumours and metastases through anti-tumour macrophages.

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Keywords: TMP195, TFMO 2 supplier, HDAC, inhibitors, activators


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