JADA82 (PCK82) is a potent KDM5A (lysine demethylase 5A) inhibitor. From patent WO2020033377A1.

CCF0058981 (CCF981), 3-chlorophenyl analogue, is a noncovalent SARS-CoV-2 3CLpro (SC2) inhibitor with an IC50 of 68 nM. CCF0058981 inhibits SC1 (SARS-CoV-1 3CLpro) with an IC50 of 19 nM. CCF0058981 has antiviral efficacy and has the potential for COVID-19 research.

RUVBL1/2 ATPase-IN-1 (compound 18) is a potent and selective inhibitor of RUVBL1/2 ATPase with IC50 values of 6.0 and 7.7 μM, respectively. RUVBL1 and RUVBL2 are highly conserved AAA ATPases (ATPases Associated with various cellular Activities) and highly relevant to the progression of cancer. RUVBL1/2 ATPase-IN-1 has the potential for the research of cancer diseases.

VB-124 is a potent and selective MCT4 inhibitor. VB124 might redirect glycolytic carbon flux into mitochondrial pyruvate oxidation. VB 124 bolcks lactate import (IC50=8.6nM), and export (IC50=19nM) in MDA-MB-231 cells that are engineers to express MCT4 as the only major plasma membrane lactate transporter.

Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer.

E-7386 (E7386) is a potent, orally active modulator of CBP/beta-catenin, disrupts the interaction and inhibits canonical Wnt signaling pathway /TCF reporter gene activity in LiCl-stimulated HEK-293 and MDA-MB-231 with IC50 of 55 and 73 nM, respectively.

PF-719 (PF719) is a potent, selective Pyk2 inhibitor with IC50 of 17 nM, displays 25-fold selectvity over FAK (IC50=469 nM); does not have significant inhibitory effects on recombinant MLCK2, p38, Akt1, or ROCK1, and very little inhibtion at Src family kinases (IC50>5 uM); selectively inhibits tyrosine phosphorylation of Pyk2 at 1 uM, but blocks both Pyk2 and FAK phosphorylation at 2.5 uM in A20 cells; reduces chemoattractant-induced migration of B-2 and MZ B cells.

IRES-J007 ia an improved IRES inhibitor that blocks IRES-hnRNP A1 binding; binds to a small pocket structure within the RRM-containing fragment of hnRNP A1 (UP1 fragment), inhibits cyclin D1 and c-MYC IRES activity to a greater extent compared with C11 (IRES-C11); significantly reduces tumor growth of GBM xenografts in mice, and markedly reduces the mRNA translational state of cyclin D1 and c-MYC transcripts combined with PP242.

Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity.

N3-PEG3-vc-PAB-MMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the peptide N3-PEG3-vc-PAB.

EGPI-1 is a potent small molecule that inhibits the translation initiation factors eIF4E/eIF4G interaction.EGPI-1 has potent antiproliferative and proapoptotic activity in multiple myeloma cells, Jurkat cells, and A549 lung cancer cell lines, inhibts A549 proliferation with IC50 of 2.61 uM, which is better than that of 4EGI-1 (IC50=58.6 uM), inhibits cancer cell growth by inhibiting eIF4E phosphorylation and inhibiting PI3K/Akt/mTOR signal pathway.EGPI-1 induces autophagy, apoptosis, G0/G1 cell cycle arrest and ROS generation in A549 cells, disrupts the mitochondrial membrane potential (∆ψ m).EGPI-1 demonstrated in vivo anti-tumor activities in A549-xenografted athymic mice (25 mg/kg/day, 50 mg/kg/day, i.p.).

LY-3537982 (LY3537982) is a highly selective and potent KRAS-G12C inhibitor, selectively inhibits growth of KRAS G12C mutant cells (IC50=1-60 nM).LY-3537982 does not inhibit growth of KRAS G12S/G13C/G12D mutant cells and WT KRAS cells (CI50>10 uM).LY-3537982 displays high selectivity for proteome-wide cysteine residues was evaluated using competitive chemical proteomics (8866 peptides).LY3537982 inhibits the growth of subcutaneous EL3187 NSCLC PDX tumors in nude mice in a dose dependent manner.LY3537982 demonstrates robust tumor regression in combination with other agents in KRAS G12C in vivo models.LY3537982 is a promising KRAS G12C inhibitor predicted to deliver >90% KRAS G12C target occupancy in the clinic.

Thalidomide-Piperazine 5-fluoride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells.

NCT58(NCT 58) is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells.

Runcaciguat is a potent soluble guanylyl cyclase (sGC) stimulator/activator..

NBI921352 is a Nav1.6 inhibitor with an IC50 value of 3.765 μM.

Inaxaplin is an apolipoprotein L1 (APOL1) function inhibitor (WO2020131807, compound 2). Inaxaplin can be used for the research of kidney disease.

NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC50 of 22.9 µM and a Kd of 54.8 nM[1].

BAY-3827 (BAY3827) is a potent, selective inhibitor of AMPK as tool compound to evaluate the therapeutic potential of AMPK inhibition in MYC-dependent tumors; strongly inhibits Acetyl-CoA carboxylase (ACC) phosphorylation in COLO 320DM and IMR-32 cells, but fails to inhibit the proliferation of cells with dysregulated c-MYC or N-MYC.

BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)[1]

Erastin 2(Erastin-2)is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter.

Benitrobenrazide is a novel selective hexokinase 2 (HK2) inhibitor, blocking cancer cells growth by targeting glycolysis.

MRTX0902 is a potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).

QN523 exhibits potent cytotoxicity in pancreatic cancer cell lines (IC50 of 0.11 μM in MIA PaCa-2 cells) and significantly delays growth of MIA PaCa-2 xenograft in NOD/SCID mice without systemic toxicity.

ERX-41 is a potent therapeutic agent targeting lysosomal acid lipase A (LIPA) and shows the mechanism of action (disruption of protein folding and induction of ER stress) that may have utility in treating patients with TNBC or other multiple solid tumors.

CID661578 is a potent inducer of β-cell regeneration, which boosts protein synthesis and regeneration by blocking MNK2 from binding eIF4G in the translation initiation complex at the mRNA cap.

IGUANA-1 is an isoform-selective guanidinyl antagonists of ALDHs, which exhibits proteome-wide target specificity and selectively blocks the growth of colon cancer spheroids and organoids.