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
BP13877	GSK126
BP13877	GSK126 is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
BP13876	GSK121
BP13876	GSK121 is an inhibitor of selective PAD4.
BP13875	GSK046
BP13875	GSK046 is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins(IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively). It has immunomodulatory activity.
BP13874	GSK 690 Hydrochloride
BP13874	GSK 690 is a reversible inhibitor of lysine-specific demethylase 1 (LSD1) (Kd: 9 nM; biochemical IC50: 37 nM).
BP13873	Molibresib
BP13873	GSK 525762A (I-BET 762) is an inhibitor of BET proteins (IC50: about 35 nM).
BP13872	GS-626510
BP13872	GS-626510 is an orally bioavailable inhibitor of BET family bromodomains (Kd: 0.59-3.2 nM for BRD2/3/4; IC50: 83 nM and 78 nM for BD1 and BD2).
BP13871	Gomisin J
BP13871	Gomisin J is a natural product and have vasodilatory activity. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells.
BP13870	Go 6983
BP13870	Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
BP13869	Gnetol
BP13869	Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of arachidonic acid (AA)-induced platelet aggregation.
BP13868	GNE-987
BP13868	GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively). GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03 nM for EOL-1 AML cell line).
BP13867	GNE-955
BP13867	GNE-955 is a potent and orally active inhibitor of pan Pim kinase (Kis: 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively).
BP13866	GNE-781
BP13866	GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).
BP13865	GNE-272
BP13865	GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.
BP13864	GNE-207
BP13864	GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).
BP13863	GNE-049
BP13863	GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).
BP13862	GNA002
BP13862	GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM).
BP13861	GN44028
BP13861	GN44028 is a hypoxia-inducible factor inhibitor of (HIF)-1 (IC50: 14 nM). GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity. However, It can not be suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
BP13860	Filgotinib
BP13860	GLPG0634(filgotinib) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
BP13859	Givinostat hydrochloride monohydrate
BP13859	Givinostat hydrochloride monohydrate is an HDAC inhibitor.
BP13858	Givinostat hydrochloride
BP13858	Givinostat hydrochloride is an inhibitor of HDAC with IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride exhibits anti-inflammatory, anti-angiogenic, and antineoplastic activities.