| DC47264 |
MS67 |
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects. |
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| DC47608 |
EZH2-IN-2
Featured
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EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity. |
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| DC47609 |
PRMT1-IN-1 |
PRMT1-IN-1 is a PRMT1 inhibitor. |
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| DC47610 |
PRMT5-IN-3 |
PRMT5-IN-3 is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents. |
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| DC47611 |
PRMT5-IN-14 |
PRMT5-IN-14 is a PRMT5 inhibitor to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations. |
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| DC47612 |
PRMT5-IN-11 |
PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range. |
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| DC47613 |
PRMT5-IN-12 |
PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5. |
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| DC47614 |
EEDi-5273
Featured
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EEDi-5273 is an exceptionally potent and orally efficacious embryonic ectoderm development (EED) inhibitor with IC50 of 0.2 nM and inhibits the KARPAS422 cell growth with IC50 of 1.2 nM. EEDi-5273 demonstrates an excellent PK and ADME profile, and its oral administration leads to complete and persistent tumor regression in the KARPAS422 xenograft model with no signs of toxicity. |
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| DC47615 |
PRMT5-IN-9 |
PRMT5-IN-9 is a novel PRMT5 inhibitor for treating cancer, with an IC50 of 0.01 μM. |
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| DC47616 |
EPZ-719
Featured
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EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases. |
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| DC47617 |
EED ligand 1 |
EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase. |
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| DC47618 |
PRMT5-IN-10 |
PRMT5-IN-10 has promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex. |
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| DC47943 |
MS33 |
MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia. |
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| DC48009 |
DCLX069 |
DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects. |
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| DC48412 |
CPI-1328 |
CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM. |
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| DC48413 |
PRMT5-IN-15 |
PRMT5-IN-15 is a PRMT5 inhibitor with an IC50 value of 0.84 nM. |
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| DC48414 |
EZH2-IN-6 |
EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor activity. |
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| DC50233 |
(S)-HH2853 |
(S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent EZH1/2 dual inhibitor with an IC50 of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases. |
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| DC50234 |
(R)-HH2853 |
(R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201). |
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| DC50236 |
MC4355 |
MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC). |
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| DC70095 |
NSD1 inhibitor BT5
Featured
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NSD1 inhibitor BT5 is a covalent, small molecule inhibitor of NSD1 histone methyltransferase with IC50 of 1.4 uM, shows no covalent binding to NSD2. |
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| DC70178 |
AH237 |
AH237 (AH-237) is a potent and selective inhibitor for PRMT4 and PRMT5 with IC50 of 2.8 and 0.42 nM, respectively.AH237 (AH-237) displayed over 50-fold selectivity against a panel of 41 MTases such as PRMTs, PKMTs, NTMT1/2, and DNA methyltransferases (DNMTs), Its potency was also confirmed for PRMT1 (IC50 = 5.9 uM) and PRMT7 (IC50 = 831 nM). |
|
| DC70212 |
ASH1L inhibitor AS-99 |
ASH1L inhibitor AS-99 (AS-99) is a first-in-class, potent, selective inhibitor of ASH1L histone methyltransferase with IC50 of 0.79 uM.AS-99 strongly bind to the ASH1L SET domain with Kd values of 0.89 uM.AS-99 displayed no significant inhibition (>100-fold selectivity) at 50 uM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2.AS-99 inhibits the growth of leukemia cells (MV4;11, MOLM13, and KOPN8) harboring different MLL1 translocations with the GI50 values of 1.8-3.6 uM, showed a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, without toxicity in normal cells.AS-99 impairs transcriptional program of MLL fusion proteins and reduces leukemia burden.AS-99 reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice. |
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| DC70238 |
BAY-155 |
BAY-155 (BAY155) is a novel, potent and selective menin-MLL inhibitor with binding IC50 of 8 nM, 10-fold better compared to that of MI-503;
BAY-155 demonstrated a significantly enhanced selectivity profile compared to MI-503 in a panel of assays covering numerous safety pharmacology-relevant targets including GPCRs, ion channels and transporters.
BAY-155 shows anti-proliferative activity in a large cell line panel, exhibits specific therapeutic activityin AML/ALL models. |
|
| DC70269 |
BR-001 |
BR-001 (BR001) is a potent, selective, allosteric inhibitor of EED subunit of PRC2 complex, disrupts EED-H3K27me3 interaction (IC50=4.5 nM).BR-001 directly binds to EED in the H3K27me3-binding pocket, BR-001 significantly increases the thermal stability of EED in thermal shift assay.BR-001 is selective for EED, has no activity against 371 wild-type kinases.BR-001 significantly reduced the cellular H3K27me3 level and also exhibited a strong antiproliferative effect in Karpas 422 cells.BR-001 inhibited proliferation of DLBCL cells and tumor growth, and upregulated target genes expression.BR-001 has potent antitumor efficacy in vivo, modulates immune response to suppress syngeneic CT26 colon tumor. |
|
| DC70341 |
DC541 |
DC541 (DC 541) is a potent, selective peptidomimetic inhibitor of Protein N-terminal methyltransferase NTMT1 with IC50 of 0.34 uM;
DC541 exhibits over 300-fold selectivity to several methyltransferases.
DC541 inhibited funtions the cellular α-N-terminal methylation level of regulator of chromosome condensation 1 (RCC1, IC50 value of 30 μM) in human colorectal cancer HT29 cells. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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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