WM-1119(WM1119) is a highly potent, selective inhibitors of KAT6A and KAT6B.

ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively.

EX 527 is a potent and selective SIRT1 inhibitor with IC50 of 38 nM, exhibits >200-fold selectivity against SIRT2 and SIRT3.

YC8-02 is a small molecule mitochondrial-targeting SIRT3 inhibitor with IC50 of 0.53 uM.YC8-02 inhibits SIRT1 and SIRT2 with IC50 of 2.8 and 0.062 uM in in vitro biochemical assays.YC8-02 manifested increased ratio of mitochondria to total cell concentration, as measured by mass spectrometry in purified mitochondria extracts and total cell lysates.YC8-02 increased mitochondrial protein acetylation, inhibited GDH activity and induced autophagy in DLBCL cells.YC8-02 could phenocopy the effects of SIRT3 depletion.YC8-02 (30 mg/kg) caused regression of the tumors in DLBCL xenografts, with no evidence of discomfort or weight loss.

XY153 is a potent, BD2-selective BET inhibitor with IC50 of 0.79 nM for BRD4 BD2, 354-fold selectivity over BRD4 BD1.XY153 displays 6-fold BRD4 BD2 domain selectivity over other BET BD2 domains.XY153 displayed potent antiproliferative activity against multiple tumor cell lines, especially MV4-11 (IC50=0.55 nM), also demonstrated good metabolic stability in vitro.

XP-524 (XL-223, XP524) is a potent, dual-BET/EP300 inhibitor, inhibits BRD4-BD (IC50=5.8 nM) and BRD4-BD2 (IC50=1.5 nM).XP-524 binds strongly to and inhibits EP300 and CBP proteins with IC50 of 28 and 116 nM, respectively.XP-524 (XL-223) showed high potency and selectivity (Kd < 1 nM) across BET family proteins. Selectivity for BRD proteins over all other bromodomain proteins was >400-fold.XP-524 significantly decreased expression of Myc pathway oncogenes such as c-MYC and n-MYC, increased expression of CDKN1B, a tumor suppressor that prevents the activation of the cyclin-D/CDK4 complex, and also reduced expression of cyclin-D (CCND1) itself.XP-524 showed increased potency and superior tumoricidal activity than the benchmark BET inhibitor JQ-1 in vitro, with comparable efficacy to higher-dose JQ-1 combined with the EP300/CBP inhibitor SGC-CBP30.XP-524 prevented KRAS-induced, neoplastic transformation in vivo and extended survival in two transgenic mouse models of aggressive PDAC.

WDR5 inhibitor 41 is a potent, selective and orally bioavailable WDR5 WIN-site inhibitor with TR-FRET Ki value of <0.02 nM, inhibits cell proliferation of MV4:11 and MOLM-13 with IC50 of 13 and 27 nM, respectively.WDR5 inhibitor 41 is well tolerated in mice by both iv and po dosing and showed no clinical sign of abnormalities suggesting an enhanced safetyprofile for the series.

UM-002 is a highly potent, selective, brain penetrant BRD4 bromodomain inhibitor with IC50 of 8.8 and 2.4 nM for BRD4-1 and BRD4-2, respectively.UM-002 is more potent than JQ1 at inhibiting BRD2-1, BRD4-1, and BRD4-2.UM-002 reduces GBM cell proliferation more than JQ1, or the brain penetrant BET inhibitor MK-8628.UM-002 not affect the enzymatic activity of histone deacetylases, histone acetyltransferases.UM-002 inhibits GBM cell proliferation in vitro with EC50 of 0.13 and 0.24 uM for GBM22 cells and GBM39 cells, repectively.UM-002 reduces proliferation of GBM cells co-cultured with cerebral brain organoids, reduces the expression of cell-cycle related genes in vivo and reduces the expression of invasion related genes within the non-proliferative cells present in tumors.

UBD253 (SGC-UBD253) is a potent, selective ubiquitin chemical probe for ubiquitin binding domain of HDAC6 with Kd of 84 nM (SPR), inhibits the HDAC6-ISG15 interaction (EC50=1.9 uM, nanoBRET).UBD253 (SGC-UBD253) displays little to no affinity for other USPs (>100-fold selectivity). SGC-UBD253 potently (<100 nM) binds HDAC6-UBD (ubiquitin binding domain), decreases the interaction between full-length HDAC6 with ISG15.

TDI-6118 is a potent, selective brain-penetrant EZH2 inhibitor with IC50 of 14 nM, inhibits cellular H3K27me with IC50 of 580 nM.

TDI-11904 is a highly potent, and peripherally active EZH2 inhibitor.

TC-5115 (TC5115 ) is a potent, selective inhibitor of MLL1 SET domain with IC50 of 15 nM, 48 times more potent than the pan-methyltransferase inhibitor SAH.

Targapremir-200c (TGP-200c) is a structure-specific, small molecule inhibitor of miR-200c precursor (pre-miR-200c), binds to the Dicer site of pre-miR-200c with Kd of 50 nM.TGP-200c inhibits Dicer processing of pre-miR-200c with IC50 320 nM, selectively engages pre-miR-200c in cells.TGP-200c potently inhibits miR-200c biogenesis selectively across the miRnome and modulates the downstream miR-200c pathway.TGP-200c selectively inhibits miR-200c over other miR-200 family members by recognizing the 1x1 UU internal loop unique to pre-miR-200c and an adjacent AU base pair simultaneously.TGP-200c selectively rescues a miR-200c-mediated phenotype in MIN6 cells, induces anti-apoptotic phenotype, modulates various T2D-related pathways, including insulin signaling and metabolism, represses pro-cell death factors and promotes β cell survival in specific ways.

SW2_152F (SW2 152F) is a potent, selective, cell permeable CBX2 chromodomain probe, binds to the N-terminal chromodomain (ChD) with Kd of 80 nM.SW2_152F displays 24-1,000-fold selectivity for CBX2 ChD over other CBX paralogs (CBX4/6/7/8) in vitro.SW2_152F is cell permeable, selectively inhibits CBX2 chromatin binding in cells, and blocks neuroendocrine differentiation of prostate cancer cell lines in response to androgen deprivation.

SW-101 (SW101) is a potent, selective HDAC6 inhibitor with IC50 of 0.7 nM, >200-fold selectivity over HDAC1/2/3.SW-101 possesses excellent HDAC6 potency and selectivity, together with markedly improved metabolic stability and druglike properties compared to SW-100.SW-101 treatment elevates the impaired level of acetylated α-tubulin in the distal sciatic nerve, counteracts progressive motor dysfunction, and ameliorates neuropathic symptoms in a CMT2A mouse model bearing mutant MFN2.

SRX3262 is a potent, triple BTK/PI3K/BRD4 inhibitor.

SRX3212 (SRX 3212) is a potent, dual BRD4/PI3Kα inhibitor with IC50 of 3.7 nM (BRD4 BD1) and 32 nM (BRD4 BD2), IC50 of 22 nM for PI3Kα.SRX3212 demonstrated strong anti-cancer activity in cyclinD1 dependent mantle cell lymphoma cell lines (Jeko-1, Mino and Z138), a colon carcinoma cell line (HCT116), a MYCN amplified p53 mutated neuroblastoma cell line (SKNBE2) and a PTEN mutated prostate cancer cell line (PC3), with nanomolar to low micromolar IC50 values.

SMYD3 inhibitor 29 is a highly potent, selective, covalent inhibitor of histone methyltransferase SMYD3 with IC50 of 11.7 nM.SMYD3 inhibitor 29 exhibits high potency by inhibiting SMYD3's enzymatic activity and showing antiproliferative activity against HepG2 in 3D cell culture (GI50=1.04 uM).SMYD3 inhibitor 29 inhibits cellular MAP3K2 methylation.SMYD3 inhibitor 29 displayed high selectivity when tested against a panel of methyltransferases, namely, SMYD1-2, G9a, PRDM9, and PRMT5.

SKI-73 is a CARM1 chemical probe with pro-drug properties, can readily penetrate cell membranes and then be processed into two active CARM1 inhibitors.SKI-73 (10 uM) fully suppresses the methylation of BAF155 Arg1064 in MCF-7 cells.SKI-73 inhibits in vitro invasion but not proliferation of breast cancer cells ( MDA-MB-231 cell, EC50=1.3 uM).SKI-73 recapitulates the anti-invasion effect of the genetic perturbation of CARM1.Either CARM1 knockout or CARM1 inhibition with SKI-73 alters the epigenetic plasticity in a proliferation-independent manner by replacing the most invasion-prone subpopulation with the non-invasive subpopulation(s) to suppress the invasive phenotype.

SJ018 (SJ-018) is a potent, highly selective BET BD2 inhibitor with Kd of 14 nM (BRD2-BD2), 67-fold selectivity over BRD2-BD1. SJ018 is more effective than JQ1 in increasing FRAP in cells, potently inhibits MV4-11 cell growth with GI50 of 2-3 nM (Days3-7).

SIRT6 activator CL5D is a novel small-molecule activator of SIRT6 deacetylation, stimulates 4-fold activation of SIRT6 (1 uM) against H3K9ac (20 uM) at 3 uM.CL5D demonstrate competitive inhibition with Ki of 13.4 uM.CL5D exhibited time-dependent deacetylation at H3K9 by SIRT6 in HEK293T cells.

SIRT5 inhibitor 32 is an efficient, cellularly active small molecule that targets SIRT5.SIRT5 inhibitor 32 inhibits cell growth of SIRT5-dependent AML cell lines SKM-1, OCIAML2 and MOLM-13 with IC50 of 9, 20, and 24 uM, respectively.SIRT5 inhibitor 32 is also shown to inhibit SIRT5 in HeLa cells by using an assay that produce in-cell fluoresence in response to SIRT5 activity in the mitochondria.SIRT5 inhibitor 32 displays cytoselective toxicity towards SIRT5-dependent AML cells (SKM-1) over HEK293T cells in culture.

SIRT3 inhibitor 8 is a SIRT3 selective inhibitor with IC50 of 6 uM, 6.8- and 5.3-fold selectivity for SIRT3 versus SIRT1 and SIRT2.SIRT3 inhibitor 8 reduced DLBCL cell viability and triggered activation of autophagy.

SIRT2 inhibitor 56 is a potent selective SIRT2 inhibitor with IC50 of 780 nM.SIRT2 inhibitor 56 displays >300 to >800-fold selectivity over SIRT1 and 3, respectively.SIRT2 inhibitor 56 dose-dependently increases tubulin acetylation in treated non-small cell lung cancer cell line NCI-H460.SIRT2 inhibitor 56 shows cytotoxicity in in B-cell lymphoma and other cancer cell lines (Raji cell IC50=9.1 uM).SIRT2 inhibitor 56 induces apoptosis and shows anti-proliferation effect in OCI-Ly8-LAM53 (OCI) cells.

SIRT2 inhibitor 55 is a potent and selective SIRT2 inhibitor with IC50 of 250 nM.SIRT2 inhibitor 55 displays >300 to >800-fold selectivity over SIRT1 and 3, respectively.SIRT2 inhibitor 55 dose-dependently increases tubulin acetylation in treated non-small cell lung cancer cell line NCI-H460.SIRT2 inhibitor 55 shows cytotoxicity in in B-cell lymphoma and other cancer cell lines (Raji cell IC50=11.9 uM).

SGC8158 (SGC-8158) is a potent, selective, and SAM-competitive inhibitor of PRMT7 with IC50 of <2.5 nM, the active component of it's cell permeable prodrug SGC3027.

SGC6870N is the negative control of SGC-6870 (R-isomer), which is a potent, selective, cell-active PRMT6 inhibitor.

SGC6870 (SGC-6870 (R-isomer)) is a potent, selective, cell-active PRMT6 inhibitor with IC50 of 77 nM.SGC6870 displays outstanding selectivity for PRMT6 over a broad panel of other methyltransferases and nonepigenetic targets.SGC6870 binds to a unique, induced allosteric pocket of PRMT6.SGC6870 engages PRMT6 and potently inhibits its methyltransferase activity in cells.SGC6870 is a well-characterized PRMT6 chemical probe and a valuable tool for further investigating PRMT6 functions in health and disease.

SGC3027N (SGC-3027N) is a negative control compound for SGC3027, shows markedly less potent (14 uM) against PRMT7 and other protein methyltransferases.

PTG-0861 (JG-265) is a novel potent, selective HDAC6 inhibitor with IC50 of 5.92 nM, >36-fold selectivity over other HDACs.PTG-0861 (JG-265) displays HDAC6 cellular target engagement with EC50 of 0.59 uM (ELISA), has in vitro and cellular selectivity superior to HDAC6-selective inhibitor citarinostat (ACY-241).PTG-0861 (JG-265) demonstrates potency against several blood cancer cell lines (e.g. MV4-11, MM1S), whilst showing limited cytotoxicity against non-malignant cells and CD-1 mice.PTG-0861 (JG-265) exihibits promising in vitro pharmacokinetics achieved with good safety profile in cells and in vivo.