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.

Jun9-62-2R (dichloroacetamide) is a selective covalent Mpro inhibitor with IC50 of 0.43 μM and viral replication with EC50 of 2.05 μM in Caco2-hACE2 cells. Jun9-62-2R (dichloroacetamide) is highly selective toward Mpro and does not inhibit the host calpain I, cathepsins B, K, L, caspase-3, and trypsin. The widely used antibiotic chloramphenicol contains the dichloroacetamide, suggesting Jun9-62-2R might be tolerated in vivo.

BIIB091 is a novel reversible, selective, potent BTK inhibitor with Kd of 0.07 nM.

DNDI-6148 acts principally through the inhibition of Leishmania cleavage and polyadenylation specificity factor (CPSF3) endonuclease for the treatment of visceral leishmaniasis (VL).

MK-4688 is an efficient inhibitor of the HDM2-p53 protein-protein interaction.

Carcainium chloride (QX 572) is a quaternary derivative of the local anesthetic Lidocaine. Antitussive effect.

TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.

Sovilnesib(AMG650) is a kinesin-like protein KIF18A inhibitor (WO2020132648). Sovilnesib can be used for the research of cancer.

Hydroxy-PEG10-Boc is extacted from patent CN108707228 (example 0024). Hydroxy-PEG10-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG10-Boc can be conjugated to Paclitaxel or docetaxel.

Val-Cit-PAB-MMAF is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAF contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF.

SphK1&2-IN-1 is a SphK inhibitor targeting to SphK1 and SphK2. SphK1&2-IN-1 has thermal stability.

c-Met-IN-15 (compound S3) is a c-Met kinase inhibitor. c-Met-IN-15 inhibits c-Met kinase activity of 21.1% at the concentration of 10 μM.