M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM[1].
HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity[1][2].1-Naphthohydroxamic acid can induce tubulin acetylation[3].
dBRD9 dihydrochloride is a potent and selective degrader (PROTAC) of BRD9 with IC50 of 56.6 nM in MOLM-13 cells.dBRD9 is composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide.dBRD9 does not degrade BRD4 or BRD7 at concentrations up to 5 uM.dBRD9 exhibits antiproliferative effects in human AML cell lines.
JAK1-IN-11 (compound 11) is a potent inhibitor of JAK，with IC50s of 0.02 nM (JAK1)，and 0.44 nM (JAK2)，respectively. JAK1-IN-11 has high selectivity against JAK1 over JAK2[1].
TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC50s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease[1].
DKFZ-748 is a selective HDAC10 inhibitor (pIC50=7.66), and shows anti-tumor activity[1].
Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87±10 μM and 0.51±0.041 μM for BD1 and BD2, respectively.
CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.IC50:0.03±0.01μM (CBP/EP300)[1]IC50:11.0±0.6 μM(BRD4)[1]CPI-637, which demonstrated substantial biochemical potency that was confirmed by isothermal titration calorimetry. A cocrystal structure of CPI-637 in the CBP bromodomain indicated that the compound recapitulated the key hydrogen bonding interactions observed with the parent compound, with the substituted indazole filling space above Pro1110 and the Pro/Arg cleft . As expected, CPI-637 was also potent against EP300, and its opposite enantiomer displayed a >200-fold loss in potency. The biochemical potency of CPI-637 translated well into cells (CBP BRET EC50 = 0.3 μM), and the compound demonstrated a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50 = 11.0 ± 0.6 μM).CPI-637 was also highly selective against other bromodomains (detailed list in the Supporting Information), displaying substantial biochemical activity only against BRD9, which is acceptable, since inhibition of the BRD9 bromodomain has not been shown to produce a pronounced cellular phenotype . In a cellular assay, CPI-637 inhibits the expression of MYC, a transcription factor widely expressed in human cancer,with an EC50 of 0.60 μM, providing an orthogonal measure of the target engagement of the compound .The inactive enantiomer of CPI-637 displayed an EC50 in the same assay of >10 μM.[1]
DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. DNMT-IN-1 shows antiproliferative active[1].
Anticancer Agent 43 is a potent anticancer agent. Anticancer Agent 43 induces apoptosis by caspase 3, PARP1, and Bax dependent mechanisms. Anticancer Agent 43 induces DNA damage[1].
RK-582 is an orally efficacious spiroindolinone-based tankyrase inhibitor for the treatment of colon cancer. It exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered.
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to treat MLL leukemia[1].
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HADC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion[1].
SIRT1-IN-3 (compound 3j) is a potent and selective SIRT1 inhibitor, with an IC50 of 4.2 μM[1].
RBN-3143 is a potent and selective PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of inflammation[1].
KDM4-IN-3 is a KDM4 inhibitor that exhibits improved potency in biochemical assays, is cell-permeable, and kills prostate cancer cells at low micromolar concentrations.
BET-IN-10 is a BET inhibitor with anticancer effects. BET-IN-10 inhibits the cell growth of MV4-11 cells with an IC50 of 26.5 nM (WO2022012456A1; example 6)[1].
Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively[1].
ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader based on PROTAC technology with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively.
Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. Phoenixin-20 promotes neuronal mitochondrial biogenesis via CREB-PGC-1α pathway. Phoenixin-20 has anxiolytic effect[1][2][3].
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer[1].
YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells[1].
BET-IN-4 is a potent BET bromodomain protein (BRD4) inhibitor, with an IC50 of ≤ 1 μM[1].
JQ-35, (S)- is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity.
BYK204165 is a potent PARP inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1[1].
BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury[1].
Metformin D6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5) (extracted from patent WO2019246570A1)[1].