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TMP195

  Cat. No.:  DC10210   Featured
Chemical Structure
1314891-22-9
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More than 5000 active chemicals with high quality for research!
Field of application
TMP195 is the most potent and selective class IIa HDAC inhibitor.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1314891-22-9
Chemical Name: N-[2-Methyl-2-(2-phenyloxazol-4-yl)propyl]-3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzamide
Synonyms: TMP-195,TMP195,TMP 195
SMILES: CC(C)(CNC(=O)C1=CC=CC(=C1)C2=NOC(=N2)C(F)(F)F)C3=COC(=N3)C4=CC=CC=C4
Formula: C32H19F3N4O3
M.Wt: 456.42
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with an IC50 of 300 nM.
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[2].
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[1]. 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)[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC3110 CUDC-907 (PI3K/HDAC InhibitorI) CUDC-907 (PI3K/HDAC Inhibitor I) is a dual PI3K and HDAC inhibitor for PI3Kɑ, HDAC1, HDAC2, HDAC3 and HDAC10 with IC50 of 19 nM, 1.7 nM, 5 nM, 1.8 nM and 2.8 nM, respectively.
DC8252 Vorinostat (SAHA) Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.
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DC6303 Tubastatin A HCl Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
DC6304 Tubastatin A Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
DC5178 Tubacin (BML-GR362) Tubacin is a selective inhibitor of HDAC6 via inhibition of the second deacetylase domain (DD2).
DC8134 Trichostatin A (TSA) Trichostatin A (TSA) is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM; HDAC8 is the only known member of the HDAC-family that is not affected by TSA.
DC7716 TMP269 TMP269 is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs.
DC10210 TMP195 TMP195 is the most potent and selective class IIa HDAC inhibitor.
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