耗材描述
TMP195
产品活性:TMP195是选择性的IIa类组蛋白脱乙酰酶 (HDAC) 抑制剂,对HDAC4,HDAC5,HDAC7,HDAC9的 Ki 值分别为59,60,26,5 nM。
产品来源: https://www.medchemexpress.cn/TMP195.html
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:HDAC
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.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Targeted Diversity Library | Anti-Liver Cancer Compound Library | Osteogenesis Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | Anti-Hematopathy Compound Library | Multi-Target Compound Library | Bioactive Compound Library Max | Trichostatin A | Vorinostat | 4-Phenylbutyric acid | Valproic acid | Sulforaphane | Panobinostat | Entinostat | Romidepsin | Tucidinostat | RGFP966 | Belinostat | Ricolinostat | Tubastatin A | Carbamazepine | Mocetinostat | Theophylline | ITSA-1 | Tasquinimod | Santacruzamate A | LMK-235 | TMP269 | Quisinostat | Fimepinostat | Tubacin | PCI-34051 | FT895 | Pyroxamide
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