| DC70452 |
GSK217 |
GSK217 (GSK-217) is a potent, highly selective BET BD2 inhibitor with pIC50 of 7.5 (BRD4 BD2), 300-fold selectivity over BRD4 BD1. |
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| DC70462 |
GSK3543105 |
GSK3543105 is a potent, selective, non-nucleoside inhibitor of DNMT1 with IC50 of 33 nM. |
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| DC70463 |
GSK3735967 |
GSK3735967 is a potent, selective, non-nucleoside inhibitor of DNMT1 with IC50 of 40 nM. |
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| DC70466 |
GSK549
Featured
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GSK549 (GSK-549) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.8 (BRD4 BD2), 1150-fold selectivity over BD1. |
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| DC70471 |
GSK737 |
GSK737 (GSK-737) is a potent, highly selective BET BD2 inhibitor with pIC50 of 7.3 (BRD4 BD2), 200-fold selectivity over BRD4 BD1. |
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| DC70478 |
HDAC3 inhibitor PT3
Featured
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HDAC3 inhibitor PT3 is a novel potent, selective, BBB-permeable HDAC3 inhibitor.PT3 exhibited higher selectivity for HDAC3 over HDAC1, HDAC6, and HDAC8 compared to the reference compound CI994.PT3 upregulated H3K9 acetylation, CREB 1, BDNF, TRKB, Nr4a2, c-fos, PKA, GAP 43 and MMP9 expression in mouse neuronal (N2A) cells.PT3 significantly improved the discrimination index in C57/BL6 mice in the novel object recognition (NOR) model, significant increased in H3K9 acetylation in hippocampus.PT3 upregulated CREB 1, BDNF, TRKB, Nr4a2, c-fos, PKA, GAP 43, PSD 95 and MMP9 expression in mice treated with PT3. |
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| DC70508 |
IMP-1575 |
IMP-1575 (IMP1575) is a potent, selective Hedgehog acyltransferase (HHAT) inhibitor with Ki/IC50 of 38 nM/0.75 uM (Acyl-cLIP assay).IMP-1575 is the first sub-micromolar small-molecule HHAT inhibitor reported to-date.IMP‐1575 (50-0.023 μM) was therefore analyzed for effects on HHAT kinetics at varying Pal‐CoA concentrations (50–0.19 μM).IMP-1575 is a chemical tool and methodology to provide insight into HHAT which may expedite future studies and drug discovery efforts against this important target class. |
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| DC70513 |
iP300w |
iP300w is a potent p300/CBP inhibitor, inhibits p300-mediated H3K9 acetylation with IC50 of 33 nM in HTRF assay.iP300w diminishes DUX4-induced toxicity and inhibits DUX4-mediated transcription.iP300w blocks DUX4-induced H3 acetylation and prevents the increase in expression of DUX4 target genes, erases the DUX4-mediated transcriptional fingerprint in FSHD myoblasts.iP300w impairs DUX4-mediated transcription in vivo in the iDUX4pA FSHD mouse model. |
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| DC70516 |
IRBM6 |
IRBM6 (Class I HDAC-IN-6) is a potent, class I selective HDAC inhibitor with EC50 of 50 nM (HeLa cellular), HDAC1/2/3 IC50 of 1.7/2.8/1.1 nM.IRBM6 weakly inhibits HDAC6 (IC50=177 nM) and is inactive at 5 uM against HDACs 4-7.IRBM6 showed a potent inhibitory effect on the growth TC-797s and two additional NUT carcinoma (NC) cell lines, PER-403, and 10-15.IRBM6 induces a transcriptional program of differentiation in NC cells, demonstrated large-scale changes in gene expression that were significantly enriched with differentiation gene sets and depleted of pro-growth gene sets, including those of MYC and E2F targets.IRBM6 repressed growth and induced differentiation of NUT carcinoma (NC) cells in proportion to inhibition of NUT transcriptional activity. |
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| DC70534 |
KA2507
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KA2507 (KA-2507, KA 2507) is a potent and selective inhibitor of HDAC6 with IC50 of 2.5 nM, >300-fold selectivity over other HDACs.KA2507 demonstrated cellular potency (IC50=150 nM) in a cellular assay measuring induction of acetylated α-tubulin, a marker of HDAC6 inhibition.KA2507 displays antiproliferative effects against a set of 93 human cancer cells with IC50 of 2-30 uM.KA2507 inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model. |
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| DC70537 |
KDOBA67 |
KDOBA67 is a novel cell-permeable inhibitor of H3K27 lysine demethylase KDM6A/B, inhibits TBXT expression chordoma cell lines.KDOBA67 displayed in vitro inhibitory activity in the low micromolar range with IC50 values of 2 to 5 uM in various chordoma cell lines, leading to induction of apoptosis.H3K27 demethylase inhibition via KDOBA67 alters chromatin state at TBXT and inhibits its expression.TBXT was a KDM6A/B target gene, and chromatin changes at TBXT following KDOBA67 treatment were associated with a reduction in TBXT protein levels.KDOBA67 treatment downregulated expression of a network of transcription factors critical for chordoma survival and upregulated pathways dominated by ATF4-driven stress and proapoptotic responses. |
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| DC70566 |
LM146 |
LM146 (LM-146) is a potent and selective inhibitor of pan-PB1 bromodomains (Polybromo-1 protein, PBRM1 or BAF180), binds to PB1(2), PB1(5), and SMARCA2B with KD values of 110, 61, and 2100 nM, respectively.LM146 displayed 34-fold selectivity profile for PB1(5) over SMARCA2, showed no binding to any bromodomains outside the sub-family VIII at 10 uM.PB1 (Polybromo-1 protein) is a component of the BRG1/BRM-associated factor (PBAF) complex, a human analog of the yeast switch/sucrose non-fermenting (SWI/SNF) complex. PB1 is a unique epigenetic reader that contains six distinct bromodomains, while other known bromodomain-containing proteins possess at most two bromodomains. The multi-subunit PBAF complex contains three bromodomain-containing proteins (BCPs): BRD7, a member of the sub-family IV, and SMARCA4 (also known as BRG1) and PB1, two members of the sub-family VIII. |
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| DC70572 |
LSH-A54 |
LSH-A54 is a potent, class I selective HDAC inhibitor with IC50 of 26.2 nM (HDAC1) and 59.3 nM (HDAC2);
LSH-A54 displays no significant inhibition against HADC3/6 (IC50>10 uM).
LSH-A54 exhibits antiproliferative properties against breast cancer cell lines T-47D (IC50=1.58 uM), MCF-7 (IC50=1.32 uM) and BT-474 (IC50=2.55 uM).
LSH-A54 attenuates cell migration significantly in wound healing assay and comparably to the pan-HDACi vorinostat, whereas the HDAC1-3 selective HDACi entinostat has no significant effect on cell migration.
LSH-A54 reduced the number of colonies significantly in clonogenic survival assay compared to entinostat and showed comparable activity to pan-HDACi vorinostat. |
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| DC70598 |
MINA53 inhibitor 9 |
MINA53 inhibitor 9 is a first in class, potent, selective MINA53 inhibitor with IC50 of 1.6 uM, selective over NO66, KDM4-6 and other JmjC oxygenases. |
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| DC70599 |
miR-21 inhibitor 12
Featured
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miR-21 inhibitor 12 (miR-21-IN-12) is a small molecule inhibitor of microRNA-21 expression and inhibit miR-21 transcription.miR-21-IN-12 inhibited transcription of the miR-21 gene resulting in significant reductions in primary and mature miR-21 levels.miR-21-IN-12 demonstrated cytotoxicity in a cervical cancer cell line via induction of apoptosis and was capable of reducing microtumor formation in a long-term clonogenic assay.miR-21-IN-12 shows some level of selectivity for miR-21 and is not a general miRNA pathway inhibitor. |
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| DC70600 |
MJM-1 |
MJM-1 is a small-molecule brain-penetrant HDAC inhibitor that increases the overall level of histone 3 (H3) acetylation in prostate cancer cell line.MJM-1 injected intraperitoneally (i.p.) crossed the BBB in mice and could be detected in the hippocampus, a brain region that mediates memory.MJM-1 (post-training i.p. administration) enhanced hippocampus-dependent spatial memory consolidation in male mice. |
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| DC70614 |
MO-I-500 |
MO-I-500 is a pharmacological inhibitor of m6A demethylase FTO, inhibits purified FTO demethylase catalyzing demethylation with IC50 of 8.7 uM.MO-I-500 treated cells exhibited a global increase in RNA methylation.HeLa cells treated with 25 μM MO-I-500 for 24 hours showed a 9.3% increase in N6-methyl-adenosine content in total RNA.MO-I-500 treatment caused a dramatic (>95%) inhibition in colony formation in SUM149-Luc cells.MO-I-500 modulates various microRNA in treated (25uM) HeLa cells.MO-I-500 treatment also led to decreased levels of FTO and IRX3 proteins in the SUM149 cells, with relatively little effect on cell growth.MO-I-500 can strongly reduce the adverse effects of streptozotocin (STZ) model of AD in human astrocytoma CCF-STTG1 cells. |
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| DC70627 |
MU1656 |
MU1656 (MU 1656 ) is a potent, highly selective inhibitor of histone methyltransferase DOT1L with IC50 of 2 nM;
MU1656 displays highly selectively against a panel of 37 methyltransferases.
MU1656 is more metabolically stable and significantly less toxic in vivo than pinometostat. |
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| DC70630 |
MV1035 |
MV1035 (MV-1035) is a novel small molecule that reduce U87 GBM cells migration and invasiveness, targeting m6A demethylase ALKBH5, also inhibits ALKBH2;
MV1035 directly inhibits active recombinant ALKBH5 protein and, consequently, negatively regulates CD73 protein expression without affecting CD73 mRNA transcription.
In PD-GSCs, MV1035 has a synergistic effect with TMZ in reducing cell viability and their ability to form spheres.
MV1035 is able both to reduce the expression of MGMT and to inhibit ALKBH2 activity. |
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| DC70636 |
NAH-C3-GPKK |
NAH-C3-GPKK is a potent, selective protein N-terminal methyltransferase 1 (NTMT1) bisubstrate inhibitor with Kiapp of 7 nM in endogenous proteomes.NAH-C3-GPKK also potently inhibit a methyltransferase complex HemK2-Trm112 (also known as KMT9-Trm112, IC50=0.3 uM).NAH-C3-GPKK is the first potent inhibitor for HemK2/KMT9. |
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| DC70649 |
NH4-13 |
NH4-13 is a potent, SIRT2-selective inhibitor with IC50 of 87 nM, no inhibition against SIRT1/3/5/6 (CI50>50 uM).NH4-13 (30 mg/kg) significantly impaired tumor growth in HCT-116 tumor xenograft. |
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| DC70650 |
NH4-6 |
NH4-6 is a potent, selective pan SIRT1-3 inhibitor with IC50 of 3.0/0.032/2.3 uM for SIRT1/2/3, respectively.NH4-6 does not inhibits SIRT5 and SIRT6.NH4-6 (30 mg/kg) significantly impaired tumor growth in HCT-116 tumor xenograft. |
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| DC70656 |
NN-390 |
NN-390 (NN390) is a potent, selective HDAC6 inhibitor with IC50 of 9.8 nM, >200-550-fold selectivity over other HDAC isoforms.NN-390 inhibits primary cells of treatment-refractory Group 3 MB cells (SU_MB002) with IC50 of 2.33 uM.NN-390 is the first HDAC6-selective inhibitor to show therapeutic potential in metastatic Group 3 medulloblastoma (MB), an aggressive pediatric brain tumor often associated with leptomeningeal metastases and therapy resistance.NN-390 selectively targets cell population with a 44.3-fold therapeutic margin between patient-derived Group 3 MB cells in comparison to healthy neural stem cells.NN-390 demonstrated a 45-fold increased potency over HDAC6-selective clinical candidate citarinostat. |
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| DC70663 |
NR-160 |
NR-160 (NR160) is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 30 nM, shows SI (75-1847 )over all HDAC class I isoforms.NR-160 induced α-tubulin acetylation (ac-α-tubulin) in treated acute myeloid leukemic (AML) cell line HL60, but not histone H3 (ac-H3) (a marker for the inhibition of class I HDACs).NR-160 enhances the cytotoxicity induction of bortezomib, epirubicin and daunorubicin on a panel of seven leukemia cell lines |
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| DC70668 |
NVS-BPTF-1 |
NVS-BPTF-1 is the first highly potent and selective BPTF-bromodomain inhibitor with IC50 of 56 nM in an AlphaScreen assay and Kd of 71 nM in a BLI assay.NVS-BPTF-1 displays no significant interaction in DSF screen and a BROMOscan against a panel of other human bromodomains.In HEK293 cells, NVS-BPTF-1 showed on-target activity with an IC50 of 16 nM, as measured by a nanoBRET assay.NVS-BPTF-1 did not affect the proliferation of multiple human cancer cell lines, and NVS-BPTF-1 did not affect the level of PSMB8 and PSMB9 or TAP1 and TAP2, unlike BPTF siRNA knockdown caused effect. |
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| DC70673 |
OR-S0 |
OR-S0 is a potent, selective EZH2 inhibitor with IC50 of 11 nM, weakly inhibitor EZH1 (IC50=91 nM).OR-S0 inhibits H3K27me3 in HCT116 cells with IC50 of 24 nM, inhibited the growth of KARPAS‐422 cells in a dose‐dependent manner with GI50 of 210 nM. |
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| DC70674 |
ORY-1001 |
ORY-1001 (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models. |
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| DC70693 |
PFI-5 |
PFI-5 a highly biochemically potent, selective, and cell-active SMYD2 chemical probe with IC50 of 8 nM.PFI-5 inhibits p53 methylation in MCF7 cells with EC50 of 1.3 uM, with no toxicity. |
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| DC70707 |
PRC2 EED-IN-1 |
PRC2 EED-IN-1 is a potent, selective, allosteric, orally bioavailable inhibitor of the EED subunit of histone methyltransferase PRC2 with IC50 of 44 nM (H3K27me3 inhibition).PRC2 EED-IN-1 retains efficacy against EZH2 inhibitor-resistant cell lines (Karpas 44 cell IC50=27 nM), exhibits in vivo efficacy in EZH2-driven tumors in vivo. |
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| DC70719 |
PTG-0861 |
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. |
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