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.

WAY-641966 is a anti-prion agent.

WAY-320461 is a FAK inhibitor.

ELOVL1-IN-2 is an elongation of very long chain fatty acid 1 (ELOVL1) enzyme inhibitor, ELOVL1-IN-2 shows weak ELOVL1 inhibition (IC50=21 μM) and moderate potency in a primary cellular assay (HEK293 C26 IC50=6.7 μM) .

ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2.

5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice[1].