| DC41974 |
Ac-Arg-Gly-Lys(Ac)-AMC |
Ac-Arg-Gly-Lys(Ac)-AMC is a substrate for HDAC. |
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| DC42298 |
(+)-JQ-1-aldehyde |
(+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. (+)-JQ-1-aldehyde can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains. |
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| DC42299 |
NHWD-870 |
NHWD-870 is a potent, orally active and selective BET family bromodomain and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation. |
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| DC42300 |
GSK620
Featured
|
GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 |
|
| DC42301 |
BET-IN-1 |
BET-IN-1 is a bromodomain extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0. |
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| DC42459 |
SETD2-IN-1 TFA |
SETD2-IN-1 TFA is a potent, selective and orally active of SETD2 which is a human histone methyltransferase. SETD2-IN-1 TFA has anti-proliferative effects. |
|
| DC42460 |
EPZ004777 hydrochloride |
EPZ004777 hydrochloride is a potent, selective DOT1L with IC50 of 0.4 nM. |
|
| DC42490 |
α-Hydroxyglutaric acid |
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases. |
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| DC42491 |
GSK778（iBET-BD1 dihydrochloride）
Featured
|
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. |
|
| DC43966 |
Benzyl selenocyanate |
Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. Benzyl selenocyanate is an inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an with an IC |
|
| DC44009 |
FNDR-20123 free base |
FNDR-20123 free base is an orally active, safe and a first-in-class anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations. |
|
| DC44107 |
BET bromodomain inhibitor 1 |
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity. |
|
| DC44140 |
FNDR-20123 |
FNDR-20123 is an orally active, safe and a first-in-class anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1/2/3/6/8 (IC50=25/29/2/11/282 nM) and inhibits Class III HDAC isoforms at nanomolar concentrations. |
|
| DC44514 |
MR837(ZINC30303842)
Featured
|
MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain). |
|
| DC44553 |
Pep2m, myristoylated TFA |
Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an |
|
| DC44921 |
AZ506 |
AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal. |
|
| DC44922 |
UNC2400 |
UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies. |
|
| DC45270 |
CHIC35 |
CHIC35, an analog of EX-527, is a potent and selective inhibitor of SIRT1 (IC50=0.124 µM). CHIC35 shows potential selective inhibition against SIRT1 over SIRT2 (IC50=2.8 µM) or SIRT3 (IC50>100 µM). CHIC35 has anti-inflammatory effects and can be used for CHARGE syndrome research. |
|
| DC45271 |
SRT3657 |
SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect. |
|
| DC45272 |
7-Chloro-4-(piperazin-1-yl)quinoline |
7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry. 7-Chloro-4-(piperazin-1-yl)quinolone is a potent sirtuin inhibitor and also inhibits the serotonin uptake (IC50 of 50 μM). 7-Chloro-4-(piperazin-1-yl)quinolone exhibits antimalarial activity on D10 and K1 strains of P. falciparum with IC50s of 1.18 μM and 0.97 μM, respectively. |
|
| DC45335 |
3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol |
3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol, a SIRT1 activator, exhibits significant stimulation of SIRT1 activity. Anti-tumor activity. |
|
| DC45388 |
Pomiferin |
Pomiferin (NSC 5113) acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM). |
|
| DC45559 |
5-Aza-4'-thio-2'-deoxycytidine |
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects. |
|
| DC45560 |
DCH36_06 |
DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity. |
|
| DC45561 |
NiCur |
NiCur is a potent and selective CBP HAT inhibitor with an IC50 value of 0.35 μΜ. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins. |
|
| DC45562 |
PFI-90
Featured
|
PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo. |
|
| DC45796 |
M-1211 |
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression. |
|
| DC45850 |
CSV0C018875 |
CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294. |
|
| DC45859 |
EZH2-IN-5 |
EZH2-IN-5 is a potent EZH2 inhibitor with IC50 values of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively. |
|
| DC45905 |
DDO-2093 |
DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex. |
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