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.

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).

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.

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.

LPS-123 is a covalently irreversible BTK inhibitor with an IC50 of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research.

GR63799 (GR-63799X) is a selective EP3 receptor agonist. GR63799 induces bladder overactivity. GR63799 can be used for the study of the pathophysiological mechanism of overactive bladder (OAB).

CIDD-8633 is a potent DDR2 inhibitor with an IC50 of 6.105 μM. CIDD-8633 inhibits cell migration and halts the cell cycle and induces apoptosis, significantly suppressing pancreatic ductal adenocarcinoma (PDAC) tumor growth. CIDD-8633 can be used for the study of pancreatic cancer such as PDAC.

SAR-115740 is a TRPV1 antagonist. SAR-115740 exhibits developmental toxicity in H9 cell experiments. SAR-115740 can be used for research on inflammatory conditions or neurological disorders.

BTT-3034, a sulfonamide derivative, is an α2β1 integrin inhibitor. BTT-3034 inhibits cell adhesion to rat tail collagen I with an EC50 of 160 nM and a corresponding Emaxof 86%. BTT-3034 inhibits collagen binding by an α2 variant carrying the conformationally activating E318W mutation.

CL 277082 is a potent and selective acyl CoA:cholesterol acyltransferase (ACAT) inhibitor in microsomes. CL 277082 inhibits ACAT with IC50 values of 0.14 μM for intestinal mucosal microsomes, 0.74 μM for liver, and 1.18 μM for rat adrenal. CL 277082 is a ACAT-catalyzed cholesterol esterification and cholesterol absorption inhibitor.

CL2A acid is a ADC linker for synthesis of Antibody-drug conjugates (ADCs)

4-TCPA is a potent VEGFR2 inhibitor. 4-TCPA induces apoptosis and cell cycle arrest, likely through inhibition of VEGFR2 and EGFR signaling with additional effects on the mTOR pathway. 4-TCPA can inhibit the vitality and proliferation of various cancer cell lines. 4-TCPA can be used for the study of cancers such as lung cancer, breast cancer and leukemia.

MC3935 is a LSD1 inhibitor with an IC50 of 0.52  μM for LSD1-CoREST enzymatic complex. MC3935 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. MC3935 has no significant toxicity to human cells. MC3935 can be used for schistosomiasis research.

GR 55562 is a selective 5-HT1B receptor antagonist. GR 55562 can be used for the research of nerve disease.

WYE-103914 is an orally active α7 nAChR (EC50 = 0.49 µM for rat α7 nAChR, EC50 = 0.57 µM for human α7 nAChR) agonist. WYE-103914 exhibits the ability to enhance memory in multiple cognitive models. WYE-103914 is used in combination with antipsychotic drugs. WYE-103914 can be used for research on schizophrenia.

ZnPc-O3-JQ1 is a light-triggered BRD4 degrader. Under illumination, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) that degrades BRD4. The degradation of BRD4 results in downregulation of HIF-1α, thereby counteracting the photodynamic therapy (PDT) resistance induced by tumor hypoxia. ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms.

ZnPc-amide-PEG3-C2-NH2 is a photosensitizer-linker conjugate which consists of ZnPcPs and a linker. ZnPc-amide-PEG3-C2-NH2 can be used to synthesize the photo-activated BRD4 degrader pZnPc-O3-JQ1

TFCA is a liver X receptor α (LXRα) antagonist. TFCA inhibits ligand-activated LXRα coactivation and transcriptional expression of the downstream target genes involved in fatty acid synthesis. TFCA attenuates ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRα in the liver.