U-75875 is a HIV-1 protease inhibitor. U-75875 can block Gag-Pol protein processing and viral maturation and replication. U-75875 can be used for the research of infection.

DHC-286 is a molecular glue degrader targeting GSPT1. DHC-286 recruits GSPT1 to the CRL4CRBN ubiquitin ligase complex, promoting GSPT1 ubiquitination and proteasomal degradation, inducing cytotoxicity. DHC-286 is promising for research of cancers such as acute myeloid leukemia.

MXC-017 is a blood-brain barrier (BBB)-penetrant apoptosis inducer that directly targets Vimentin (VIM). MXC-017 prevents radiation-induced glioma stem cell (GSC) formation, while promoting G0/G1 cell cycle arrest and apoptosis. MXC-017 exhibits minimal off-target effects and shows no significant cytotoxicity. MXC-017 significantly prolongs median survival when used in combination with radiation therapy in glioblastoma (GBM) mouse models.

(R)-Xanthoanthrafil is a phosphodiesterase-5 (PDE5) inhibitor. (R)-Xanthoanthrafil selectively inhibits PDE5, increasing cyclic guanosine monophosphate (cGMP) levels, leading to smooth muscle relaxation and promoting penile erection. (R)-Xanthoanthrafil can be used to study erectile dysfunction.

VHL-SNAP2-5C is a SNAP-fusion protein PROTAC degrader basing on a self-labeling protein SNAP tag. VHL-SNAP2-5C by endogenous tagging enables the visualization and the selective depletion of a SNAP-fusion protein, such as CLCa andEGFP. Pink: SNAP-fusion protein ligand.

AH081 (Compound 38) is a CK1δ/ε PROTAC degrader. AH081 is the negative control compound of AH078. AH081 has inhibitory but no degradation activity for CK1δ/ε by using an inactive stereoisomer of the VHL ligand.

(S,S,S)-AHPC is an E3 ligase ligand. (S,S,S)-AHPC can be used for synthesis of PROTAC AH081.

ABT-116 is an orally active antagonist of transient receptor potential vanilloid type 1 (TRPV1). ABT-116 has analgesic efficacy. ABT-116 can be used for the research of neurological disease.

POI-4 is a ligand for METTL3. POI-4 can be used for synthesizing PROTACs such as AF151.

sEH-H ligand 1 is a PROTAC target protein ligand that can be used to synthesize PROTAC sEH degrader-2.

E17110 is a liver X receptor β (LXRβ) agonist with an EC50 of 0.72 μM. E17110 can increase the expression of ATP-binding cassette transporter A1 (ABCA1) and G1 (ABCG1) in RAW264.7 macrophages. E17110 also reduce cellular lipid accumulation and promoted cholesterol efflux. E17110 can be used for the research of cardiovascular disease, such as atherosclerosis.

Jun6504 is an enterovirus 2C inhibitor. Jun6504 shows potent and broad-spectrum antiviral activity against multiple strains of EV-D68 (EC50 = 250 nM), EV-A71 (EC50 = 502.4 nM), and CVB3 (EC50 = 1049 nM). Jun6504 improves paralysis score and weight gain in a neonatal mouse model of EV-D68 infection. Jun6504 reduces viral titers in the spinal cord and the infected quadriceps muscle. Jun6504 can be used for EV-D68 antiviral research.

AVI-4206 is a selective Mac1 inhibitor with an lC50 of 64 nM. AVI-4206 reduces viral replication, restores an interferon response, and leads to a survival benefit in an animal model of SARS-CoV-2 infection. AVI-4206 can be used the study of SARS-CoV-2 infection.

PF-05139962 is a cyclic sulfone mTOR kinase inhibitor. PF-05139962 exhibits potent mTOR (Ki = 5 nM, pS473 IC50 = 48 nM, pS6 IC50 = 6 nM) inhibitory activity and high selectivity.

OncoFAP-GlyPro-MMAE is a FAP small molecule-drug conjugate (SMDC) with an IC50 of 0.49  nM. OncoFAP-GlyPro-MMAE consists of a FAP Ligand OncoFAP), a Tubulin inhibitor (MMAE) and a linker. OncoFAP-GlyPro-MMAE can be used for cancers like renal cancer research.

YJC-10592 is an orally active CCR-2 antagonist. YJC-10592 binds to HAS. YJC-10592 can be used in the research of asthma and idiopathic dermatitis.

NB-3 is a nicotinamide adenine dinucleotide (NAD) hydrolase SARM1 inhibitor. NB-3 intercepts NAD hydrolysis and undergoes covalent conjugation with the reaction product adenosine diphosphate ribose (ADPR). The resulting small-molecule ADPR adducts are highly potent and confer compelling neuroprotection in neurological injury.

RS-56812 is a partial agonist of the 5-HT3 receptor. RS-56812 significantly enhances the propulsive peristalsis of the colon. RS-56812 indirectly enhances cholinergic neurotransmission and improves the working memory performance of non-human primates. RS-56812 is used in research on diarrhea/colon peristalsis and cognitive disorders (such as Alzheimer's disease).

Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC50 of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS).

TLR4L 10 is a TLR4 ligand. TLR4L 10 induces cells to produce IL-6. TLR4L 10 has immunostimulatory activity.

VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC50 of 9 nM and the mutant VCP proteins with IC50 of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma.

CRBN ligand-184 is a ligand for CRBN-type E3 ubiquitin ligases. CRBN ligand-184 can be used to synthesize PROTAC AU-24118.

AP-24226 is a potent inhibitor of Scr/ABL.

RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB).

MNK1 ligand 1 (Compound 5) is a MNK1 ligand. MNK1 ligand 1 can be used for synthesis of PROTAC MNK1 degrader-1.

NSC 330770, a demethylated hydrogenated molecule, is a potent tubulin polymerization inhibitor (IC50 of 2 μM). NSC 330770 elicites GTPase activity and the formation of abnormal polymers.

dASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH).

ASK1 ligand 1 is a binding ligand for ASK1 and can be used to synthesize PROTACs such as dASK1-VHL.

DF-003 is a selective, orally active, ATP-competitive, and brain-penetrant ALPK1 inhibitor. DF-003 potently inhibits human ALPK1 and ALPK1[T237M] with IC50s value of 1.5 nM and 16 nM. DF-003 exhibits more than 860-fold selectivity over the closest kinase. DF-003 inhibits TNF, CXCL10, or CXCL8 upregulation in HEK-293 cells. DF-003 can be used for the study of retinal dystrophy, optic nerve edema, splenomegaly, anhidrosis, and headache (ROSAH) syndrome.

H-151 Alkyne (Compound H-151-AL) is a selective STING (Stimulator of interferon genes) inhibitor. H-151 Alkyne is promising for research of autoimmune diseases such as systemic lupus erythematosus, scleroderma, and autoinflammatory diseases.