Epigenetics

Epigenetics is the control of gene expression without altering the DNA sequence, including DNA methylation, genomic imprinting, maternal effects, gene silencing, nucleolus dominant, dormant transposon activation, and RNA editing. In contrast to classical genetics, which focuses on the effects of gene sequences on biological functions, epigenetics focuses on the mechanisms by which these "epigenetic phenomena" are established and maintained.

Cat. No.	Product name
BP14235	Tefinostat
BP14235	Tefinostat is a monocyte/macrophage-targeted pan HDAC inhibitor. That is cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1.
BP14234	TD-428
BP14234	TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
BP14233	TCS PIM-1 1
BP14233	TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM).
BP14232	TC-S 7009
BP14232	TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
BP14231	TC-E 5003
BP14231	TC-E 5003 is a selective inhibitor of PRMT1 with IC50 of 1.5 μM.
BP14230	Tazemetostat trihydrochloride
BP14230	Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleosome assay).
BP14229	Tazemetostat
BP14229	Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyltransferase EZH2, with potential antineoplastic activity. Upon oral administration, Tazemetostat selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27).
BP14228	Tazemetostat hydrobromide
BP14228	Tazemetostat hydrobromide is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).
BP14227	Tasquinimod
BP14227	Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
BP14226	TAS-301
BP14226	TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
BP14225	Tanshindiol C
BP14225	Tanshindiol C protects macrophages from oxLDL induced foam cell formation via activation of Prdx1/ABCA1 signaling and that Prdx1 may be a novel target for therapeutic intervention of atherosclerosis.It possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information for designing a new class of potent EZH2 inhibitors.
BP14224	Tanshindiol B
BP14224	Tanshindiol B possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information for designing a new class of potent EZH2 inhibitors. It also possesses the anti-angiogenic activity,so it can be a promising candidate for angiogenesis inhibitors.
BP14223	Talazoparib tosylate
BP14223	Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
BP14222	Talazoparib
BP14222	Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity.
BP14221	T-448
BP14221	T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
BP14220	T-448 free base
BP14220	T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
BP14219	T-3775440 hydrochloride
BP14219	T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
BP14218	SW155246
BP14218	SW155246 is a potent and selective inhibitor of DNMT1 (DNA methyltransferase 1; IC50 of 1.2 μM). SW155246 induces re-expression of the tumor suppressor geneRASSF1 in A549 cells.
BP14217	SW-100
BP14217	SW-100 is a selective histone deacetylase 6 inhibitor (IC50: 2.3 nM). It also shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays an obviously improved ability to cross the blood-brain-barrier.
BP14216	Suprastat
BP14216	Suprastat is an HDAC6 inhibitor used in silico simulations.