LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.

Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research.

Merck60 (BRD 6929, Compound-60) is a potent, selective and brain-penetrant inhibitor of HDAC1 and HDAC2 with IC50 of 1 nM and 8 nM respectively.

A potent and selective type III phosphatidylinositol 4-kinase (PI4KIIIβ) inhibitor with IC50 of 3.6 nM.

Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.

URB694 is a carbamate FAAH inhibitor that irreversibly carbamoylate the nucleophile catalytic serine in FAAH active site. URB694 exhibits antidepressant-like activity and cardioprotective effects. URB694 can be used to prepare 11C-Carbonyl-URB694 for in vivo positron emission tomography (PET) imaging studies of the brain FAAH.

PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer.

Nav1.8-IN-8 (Compound A11) is a Nav1.8 channel inhibitor. Nav1.8-IN-8 may prevent associated diseases mediated by sodium ion channels (NaV).

Aspalatone is an anti-platelet aggregator (antithrombotic) that has been shown to prolong bleeding time in the mouse model. Aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy.

CSF1R-IN-20 (compound 7a) is a CSF-1R Inhibitor with an IC50 value of 467 nM. CSF1R-IN-20 inhibits CSF-1R auto-phosphorylation.

GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.

Avenanthramide-C methyl ester is an anti-inflammatory agent and NF-κB inhibitor that inhibits the secretion of pro-inflammatory factors. Avenanthramide-C methyl ester inhibits NF-κB activation by inhibiting IKK and IκB phosphorylation and inhibiting proteasome activity.

p38-α MAPK-IN-6 (compound 3a) is a p38α mitogen-activated protein kinase inhibitor.

BFC1108 is a small molecule Bcl-2 functional converter. BFC1108 induces a conformational change in Bcl-2, resulting in the exposure of its BH3 domain both in vitro and in vivo. BFC1108 effectively induces apoptosis in Bcl-2 expressing cancers.

AChE/Aβ-IN-5 (compound AV-2) is a bifunctional inhibitor that targets AChE and auto-induced Aβ (Amyloid-β) aggregation. AChE/Aβ-IN-5 can significantly improve scopolamine- and Aβ-induced cognitive impairment in mice.

ZINC000028464438 is a selective HDAC11 inhibitor with an IC50 of 3.5 µM. ZINC000028464438 shows almost no inhibition for other HDAC subtypes.

CAY10512 is an inhibitor of NF-κB. CAY10512 can suppress the upregulation of NF-κB-sensitive proinflammatory miRNAs (miRNA-9, miRNA-125b, miRNA-146a, miRNA-155) in cerebrospinal fluid and extracellular fluid, and can be used for research on Alzheimer's disease.

ATPase-IN-3 (compound 6) is a ATPase inhibitor. ATPase-IN-3 has Gastroprotective effect in ethanol-induced gastric ulcers by contribution of anti-apoptotic (BCL-2) and tumor suppressor (P53) proteins.

HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection.

Antioxidant/anticancer agent 1 (compound 5) is a pyrimidine-derivatized Schiff base based on pyrimidine hydroxy-1-naphthaldehyde and has antibacterial, antioxidant, antifungal, and anticancer properties. Antioxidant/anticancer agent 1.

TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells.

Senexin A hydrochloride is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters.

4,2′,4′,6′-Tetramethoxychalcone is a flavonoids that can be isolated from Gnaphalium affine.

Anti-osteoporosis agent-5 (compound 189) is a potent inhibitor of the formation of osteoclasts.

Anti-osteoporosis agent-6 (compound 174) is an anti-osteoporosis agent. Anti-osteoporosis agent-6 has 14.11% inhibition rate against osteoclast formation at 10 μM.

(E/Z)-CCR-11 (Comp 12) is a selective CD38 inhibitor, with an IC50 of 20.8 μM against CD38 cyclase. (E/Z)-CCR-11 promotes increases in cellular NAD+ levels and interferon γ.

Novel inhibitor of PKM2-regulated signaling, suppressing non-glycolytic PKM2-regulated signaling in cancer cells

Ameltolide, a 4-aminobenzamide derivative, is an anticonvulsant agent which has been shown to be effective at inhibiting seizures in animal models.

AN-12-H5 intermediate-3 is an intermediate of the viral inhibitor AN-12-H5 (HY-120900) and can be used to synthesize Antibody-Drug Conjugates (ADCs).

HDAC6-IN-27 (compound 8C) is a HDAC inhibitor with IC50 vales of 15.9 nM 136.5 nM and 6180.2 nM for HDAC6, HDAC8 and HDAC1, respectively. HDAC6-IN-27 shows potent antiparasitic effects.