Comopound X1 (Xist) binds the non-coding RNA prototype Xist, specifically the RepA motif, with Kd of 0.4 μM. X1 binding reduces the conformational space of RepA, displaces cognate interacting protein factors (PRC2 and SPEN), suppresses histone H3K27 trimethylation, and blocks initiation of X-chromosome inactivation.

Compound 16 (UNC-CA94) is a reversible inhibitor of PKN3 with IC50 of 14 nM. Compound 16 (UNC-CA94) is a potential tool compound to study the cell biology of PKN3.

S3-15 selectively interrupts soluble RANKL-RANK interaction and without interfering with the membrane RANKL-RANK interaction. S3-15 exhibits anti-osteoporotic effects without causing immunosuppression.

NKTP-3 is a potent, selective, biostable, and cell-permeable cyclic d-peptide that targets NRP1 and KRASG12D with binding affinity of 116.28 nM and 50.34 nM, respectively. NKTP-3 shows good biostability and a strong cellular uptake ability and further demonstrated its antitumor effect on lung cancer with the KRASG12D mutation in vitro and in vivo.

ML901 is a specific reagent that hijacks a single aminoacyl transfer RNA (tRNA) synthetases (aaRSs) in the malaria parasite Plasmodium falciparum. ML901 inhibits the growth of the malaria parasite Plasmodium falciparum in vitro and in animals but was not toxic to human cells.

IDP-410 is a novel therapeutic peptide that target directly N-MYC protein. IDP-410 peptide acts by reducing the interaction of N-MYC with its partner MAX and favoring the degradation of the protein.

N-0385 is a novel highly potent inhibitor of TMPRSS2-like proteases (IC50 = 1.9 nM) that blocks SARS-CoV-2 VOCs (B.1.1.7, P.1, B.1.351 and B.1.617.2) and is broadly protective against infection and mortality in mice. N-0385 demonstrates potent inhibition of SARS-CoV-2 infection in Calu-3 cells with EC50 of 2.8 nM and a SI of > 10E6.

DCC-3014(Vimseltinib) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively.

VH 032 Linker 2 is a derivative of the proteolysis-targeting chimera technology (PROTAC) building block VHL ligand 1.

INCB086550 is an orally available, small molecule inhibitor of PD-L1 with potential immune checkpoint inhibitory and antineoplastic activities. In vitro, INCB086550 selectively and potently blocked the PD-L1/PD-1 interaction, induced PD-L1 dimerization and internalization, and induced stimulation-dependent cytokine production in primary human immune cells. In vivo, INCB086550 reduced tumor growth in CD34+ humanized mice and induced T-cell activation gene signatures, consistent with PD-L1/PD-1 pathway blockade. Preliminary data from an ongoing phase I study confirmed PD-L1/PD-1 blockade in peripheral blood cells, with increased immune activation and tumor growth control.

TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration.

Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily[1].

Sortin3 is a sorting inhibitor, blocking Vps16 function, one protein in the class C tethering complex, and increasing aflatoxin synthesis and export.

MS4-8107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS 48107 can readily cross the blood-brain barrier (BBB) in mice[1].

Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2[1]. Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration[2]. Zinc Protoporphyrin has anti-cancer activity[3].

RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.

BAY 6035 is a potent and selective SMYD3 inhibitor.

NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.

BI-4924 (BI 4924) is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.BI-4924 splays high selectivity against the majority of other dehydrogenase targets.

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2

ACT-541468 is a dual orexin receptor antagonist.

Sodium channel blocker. Suppresses tetrodotoxin (TTX)-resistant Na+ currents approximately twice as selectively as TTX-sensitive currents. Antinociceptive; displays analgesic effects in animal models of inflammatory and neuropathic pain.

EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50 < 0.2 nM).

ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.