BI-3802 (BI3802) is a novel and highly potent BCL6 degrader which inhibits the BTB domain of BCL6 with an IC50 of ≤3 nM; BI-3802 has demonstrated potent antitumor activity by inducing efficacious BCL6 protein degradation in several diffuse large B-cell lymphoma (DLBCL) cell lines.

MT-3014, a pyrazolo[1,5-a]pyrimidine derivative, is a novel, potent, highly selective and brain-penetrant phosphodiesterase 10A (PDE 10A) inhibitor, with IC50s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively. It was discovered based on a previous compound which was deprioritized due to concerns for E/Z-isomerization and glutathione-adduct formation at the […]

TAK-981 is a novel, potent and selective small molecule inhibitor of sumoylation with potential immune-activating and antineoplastic activities. Upon intravenous administration, TAK-981 targets and covalently binds to the small ubiquitin-like modifier (SUMO; small ubiquitin-related modifier) protein, forming an adduct with SUMO protein (TAK-981-SUMO adduct). This prevents the transfer of SUMO from the SUMO-activating enzyme (SAE) […]

TAK-828F (TAK828F) is a novel, potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist with binding IC50 of 1.9 nM and reporter gene IC50 of 6.1 nM. TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ). TAK-828F showed potent RORγt inverse agonistic activity, excellent selectivity against […]

DT-061 (also known as DT061; SMAP) is a novel, potent and orally bioavailable activator of PP2A (protein phosphatase 2A) with anticancer effects. It could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis. Treatment with DT-061, in combination with the MEK inhibitor AZD6244, resulted in suppression of both p-AKT and MYC, as well as […]

LY2794193 is a novel, highly potent and selective mGlu3 receptor agonist with Ki / EC50 of 0.927 nM / 0.47 nM; 412 nM / 47.5 nM for hmGlu3 and hmGlu2, respectively.

CI-1044 is a novel, potent and orally bioavailable PDE4 (phosphodiesterase 4) inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively. It inhibits LPS-induced TNF-alpha production in whole blood in chronic obstructive pulmonary disease (COPD) patients.

IMD-0560 is a novel and potent IKK inhibitor which suppresses heart failure and chronic remodeling after myocardial ischemia via MMP alteration.

NSC601980 exhibits anticancer activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.

Cytochalasin E, an epoxide-containing analog of cytochalasin B, is a natural product acting as an autophagy inhibitor which enhances chemotherapy-induced cell death and potently and selectively inhibits the growth of endothelial cells (IC50 < 1 nM), impairing angiogenesis and tumor growth. This cytochalasin does not inhibit glucose transport or HIV-1 protease activity. The cytochalasins are […]