| DC49600 |
PARP1/BRD4-IN-1 |
PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells. |
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| DC49602 |
BRD4 Inhibitor-17 |
BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals. |
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| DC49603 |
BRD4 Inhibitor-16 |
BRD4 Inhibitor-16 (Compound 4) is a potent inhibitor of bromodomain 4 (BRD4). Overexpression of bromodomain 4 (BRD4) is closely correlated with a variety of human cancers by regulating the histone post-translational modifications. BRD4 Inhibitor-16 represents a useful tool for explorative studies of BRD4 inhibition, such as an improved understanding of BRD4 inhibitor release-related information. |
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| DC49605 |
CREB-IN-1 TFA |
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth. |
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| DC50211 |
TFMB-(S)-2-HG |
TFMB-(S)-2-HG is a potent inhibitor of the 5'-methylcytosine hydroxylase TET2. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML). |
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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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| DC70082 |
ORY-1001 trans and cis isomers |
ORY-1001 (RG-6016) 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. |
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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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| DC70098 |
KT-531
Featured
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KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity. |
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| DC70136 |
TAF1 bromodomain inhibitor |
A potent and selective TAF1(2) bromodomain inhibitor. |
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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). |
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| DC70183 |
ALKBH5 inhibitor 3 |
ALKBH5 inhibitor 3 is a small molecule inhibitor of RNA 6-N-methyladenosine (m6A) demethylase ALKBH5, inhibits ALKBH5 RNA m6A demethylation activity with IC50 of 0.84 uM. |
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| DC70184 |
ALKBH5 inhibitor 6 |
ALKBH5 inhibitor 6 is a small molecule inhibitor of RNA 6-N-methyladenosine (m6A) demethylase ALKBH5, inhibits ALKBH5 RNA m6A demethylation activity with IC50 of 1.79 uM. |
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| 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. |
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| 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. |
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| DC70270 |
BRD4 D1 inhibitor 30 |
BRD4 D1 inhibitor 30 is a high-affinity, BRD4 D1-selective chemical probe with Kd of 18 nM, 500-fold selectivity against BRD2 D1 and BRD4 D2.BRD4 D1 inhibitor 30 down regulated inflammation, IL-8 and chemokine in cell based assays, but was unable to reduce c-Myc expression at low concentration in multiple myeloma cells. |
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| DC70271 |
BRD8 inhibitor DN02 |
BRD8 inhibitor DN02 is a first-in-class selective and cellularly active probe for NuA4 factor BRD8 (BD1) with IC50 of 34 nM, no affinity for BRD8 {BD2}, CBP, and p300. |
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| DC70279 |
BY27 |
BY27 (BD2 inhibitor BY27) is a potent, highly selective BET BD2 inhibitor with Ki of 8.9/8.2/14.2 nM for BRD2/3/4-BD2 respectively.BY27 displays 38-fold selectivity for BRD2-BD2 over BRD2-BD1.BY27 showed good antitumor activity in the MV4-11 xenograft model with an improved in vivo tolerance in mice compared with I-BET762. |
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| DC70323 |
CRCM5484 |
CRCM5484 is a potent, BET BDII-selective inhibitor with IC50 of 130/20/71 nM for BRD4-BD2/BRD3-BD2/BRD2-BD2, respectively.CRCM5484 displays 475-fold selectivity over its first bromodomain (BRD3-BD2 vs BRD3-BD1).CRCM5484 demonstrates very low activity in various cell-based assays.CRCM5484 modulates the anti-leukemic activity in combination with various FDA-approved and/or in-development drugs in a cell- and context-dependent differential manner. |
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| 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. |
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| DC70344 |
DC-CBi-22 |
DC-CBi-22 is a highly potent, selective CECR2 bromodomain inhibitor with IC50 of 8.0 nM, 24.9-fold selectivity over BPTF BRD. |
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| DC70358 |
DK1-04 |
DK1-04 is a potent, selective, cell-permeable small-molecule SIRT5 inhibitor with IC50 of 0.34 uM, shows no inhibition on SIRT1-3/6 at 83 uM. |
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| DC70359 |
DK1-04e |
DK1-04e (DK1-04 prodrug) is the prodrug of DK1-04, a potent, selective, and cell-permeable small-molecule SIRT5 inhibitor with IC50 of 0.34 uM;
DK1-04e inhibits the cellular growth of breast cancer cells by targeting SIRT5.
DK1-04e impairs mammary tumor growth in MMTV-PyMT transgenic mice and human breast cancer mouse model.
SIRT5 inhibition suppressed the transformed properties of cultured breast cancer cells and significantly reduced mammary tumor growth in vivo, in both genetically engineered and xenotransplant mouse models. |
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| DC70390 |
ENL YEATS Domain inhibitor 7 |
ENL YEATS Domain inhibitor 7 is a selective, small molecule inhibitor of ENL YEATS Domain with IC50 of 0.62 uM in inhibiting the ENL-acetyl-H3 interaction.ENL YEATS Domain inhibitor 7 displayed strong selectivity toward the ENL YEATS domain over all other human YEATS domains.ENL YEATS Domain inhibitor 7 exhibited on-target inhibition of ENL in cultured cells and a synergistic effect with the bromodomain and extraterminal domain inhibitor JQ1 in killing leukemia cells. |
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| DC70419 |
FT108 |
FT108 (FT-108) is a potent, selective HDAC6 inhibitor (IC50=26 nM) relative to other HDAC family members (HDAC3 IC50=6.68 uM and HDAC8 IC50=4.07 uM). |
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| DC70420 |
FT234
Featured
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FT234 (FT-234) is a selective HDAC11 inhibitor.FT234 demonstrated significant reduction in self-renewal stem-like SP cells with 2 uM FT234 or FT895, as well as the formation of vascular networks by SP cells at 5 uM compound treatment.FT234 significantly decreased the mRNA of Sox2 as well as its target genes like HK2 and PDK2 in SPAdh cells.FT234 compound inhibited the growth and viability by 60–80% in both A549 and H1650 cells at 5-10 uM, inhibited the viability of cancer cell lines A549 and H1650 ranged from 4.663–6.594 uM, reduced the viability of chemo-resistant cancer cells as well as chemo-insensitive CSCs.FT234 selectively prevent growth of cancer cells in presence of cancer associated fibroblasts (CAFs). |
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| DC70421 |
FTO inhibitor CS1 |
FTO inhibitor CS1 (NSC 337766) is a potent, selective small-molecule inhibitor of m6A demethylase FTO, inhibits m6A demethylation with IC50 of 142.6 nM in vitro (cell-free) assays.CS1 is highly efficacious FTO inhibitors with potent anti-leukemic efficacy againsta panel of leukemia cell lines with high FTO expression in vitro (IC50 range from 20 to 175 nM, MV4-11 IC50=58.9 nM).CS1 blocks the binding of FTO with its known target mRNAs, such as MYC, CEBPA, and RARA, notably increased global m6A abundance in AML cells, does not suppress the enzymatic activity of ALKBH5, or TET1.CS1 treatment resulted in substantially increased apoptosis and cell cycle arrest (at the G0 phase), also significantly promoted myeloid differentiation in human AML cells.FTO inhibitor CS1 substantially delayed AML progression and improved survival in AML PDX mouse model, significantly more effective than FB23-2. |
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