BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC.

BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC.

BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2).

1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.

Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity.

WW437 is a histone deacetylase (HDAC) inhibitor with potent anti-breast cancer ability in vitro and in vivo.

ZL0590 is a potent, orally active BRD4 BD1-selective inhibitor with an IC50 of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities.

HDAC-IN-28, a novel HDAC inhibitor, shows potent activities against tumor growth and metastasis

Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer.

YF479, a novel HDAC inhibitor, displays more potent anti-tumor activity in vitro and in vivo compared with hydroxamic acid (SAHA).

HDAC-IN-33 is a potent HDAC inhibitor with IC50s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity.

LW479, a novel HDAC inhibitor, could be a candidate drug for breast cancer prevention.

BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC50s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5).

SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches.

HDAC-IN-32 is a potent HDAC inhibitor with IC50s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity.

HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor.

XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma.

Cas9-IN-3 is a potent Cas9 inhibitor (IC50=28 μM). CRISPR/Cas systems have revolutionized gene editing in various species.

Phenylbutyrate is a potent histone deacetylases (HDACs) inhibitor. Phenylbutyrate can be used for urea cycle disorder research.

ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models.

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.

OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells[1].

OTS186935 (OTS-186935) is a potent, in vivo-active inhibitor of protein methyltransferase SUV39H2 with IC50 of 6.49 nM, inhibits A549 cell growth with IC50 of 0.67 uM; causes a significant growth inhibitory effect in mouse xenograft models using MDA-MB-231 breast cancer cells as well as A549 lung cancer cells, at 25 mg/kg once daily for 14 days yielded a TGI of 60.8%; attenuates the levels of H3K9me3 in A549 xenograft mouse model.

SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..

4SC-202 is an orally bioavailable benzamide and inhibitor of human class I histone deacetylases (HDACs) isoenzymes 1, 2 and 3, with potential antineoplastic activity. HDAC inhibitor 4SC-202 selectively binds to and inhibits class I HDACs leading to an acc

ACY-738 demonstrates inhibitory activity against recombinant HDAC6 with IC50 values of 1.7 nM, with respective average selectivity over class I HDACs being 100-fold.

AS 8351 induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409.

BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively).

BRD-73954 is a biochemical inhibitor histone deacetylase cancer histone modification epigenetics gene regulation small molecule HDAC6 HDAC8.

Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 and 59 μM, respectively.