VU6080824 (Compound 5s), a derivative of ML-133), is an inward-rectifier potassium channel (Kir2.1) inhibitor with an IC50 of 0.35  μM. VU6080824 has superior thallium flux and manual patch clamp (MPC) functional potency.

SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC.

Lin28 degrader MG-Lin3 is a molecular glucose degrading agent that targets the Lin28 protein. Lin28 degrader MG-Lin3 significantly reduces the Renilla luciferase signal at 100 µM. Lin28 degrader MG-Lin3 inhibits the maturation of tumor microRNA let-7. Lin28 degrader MG-Lin3 can be used for cancer research.

5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.

DJ-89 (Compound 77) is a potent soluble epoxide hydrolase (sEH) inhibitor with an IC50 value of 0.51 nM . DJ-89 inhibits sEH from hydrolyzing epoxyeicosatrienoic acids (EETs), reducing the production of pro-inflammatory substances. DJ-89 is promising for research of acute and chronic inflammatory diseases (such as rheumatoid arthritis).

LC-MF-4 is a selective FGFR3 PROTAC degrader with a DC50 of 30.89 nM in KMS-11 cells. LC-MF-4 inhibits the metabolic function of FGFR3-TACC3 fusion positive cancers with reduction of ATP synthesis and inhibition of mitochondrial biogenesis genes. LC-MF-4 has potent antitumor activity in the Ba/F3-FGFR3-TACC3 xenograft mice model. LC-MF-4 can be used for FGFR3-altered cancers like bladder cancer and urothelial carcinoma (UC) research.

AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC.

Brigatinib A is an GID4 ligand. Brigatinib A can be used for synthesizing PROTAC BCR-ABL Degrader-2.

UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia.

E3 Ligase Ligand-linker Conjugate 188 is a E3 ligase ligand-linker conjugate, used for the synthesis of AZ'3137.

PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC50 = 2.83 nM). PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML).

β-Blocker B-24/76 is a beta adrenoceptor blocker. β-Blocker B-24/76 exhibits beta 1-adrenoceptor blocking and beta 2-adrenoceptor stimulating properties. β-Blocker B-24/76 can suppress the increased ornithine decarboxylase activity in hypertrophied hearts. β-Blocker B-24/76 can be used for the research of cardiovascular disease.

Metralindole is an inhibitor of human cyclin-dependent kinase CDK2 and human protein kinase CK2 holoenzyme. Metralindole shows good potential as a non-small cell lung cancer inhibitor.

(Z)-1,2-Dimethoxy-4-(3-fluoro-2-propenyl)benzene is a fluorine analog of Methyl eugenol (ME) and is attractive to oriental fruit fly B. dorsalis.

SCH-1518291 (Compound 27) is an orally active PDE10A inhibitor. SCH-1518291 exhibits antipsychotic activity in an ADHD rat model. SCH-1518291 can be used in research on neurological disorders such as psychosis.

BRP-821 is a soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 0.4 nM. BRP-821 can be used for the researches of inflammation, cardiovascular, metabolic and neurological disease .

PGE 9262932 is a quinolone antibacterial agent. PGE 9262932 can be used for the research of infection.

WCK-1152 is a fluoroquinolone antibacterial agent. WCK-1152 is active against resistant pathogens bearing mutations of DNA gyrase and/or topoisomerase IV which also express efflux pumps. WCK-1152 can be used for the research of infection, such as respiratory infections caused by resistant pneumococci and staphylococci.

DC-756 is a fluoroquinolone antibiotic. DC-756 possesses potent activity against Gram-positive and Gram-negative pathogens comparable to Trovafloxacin, with MIC, against Ofloxacin-resistant strains 16-fold better than Trovafloxacin. DC-756 is well absorbed orally in rats and found to have good photostability. DC-756 can be used to study bacterial resistance.

Dopamine D3 receptor ligand-6 (Compound 196476) is a selective dopamine D3 receptor (D3) antagonist. Dopamine D3 receptor ligand-6 is promising for research of substance use disorders (such as opioid and psychostimulant addiction).

3-(7-Methoxy-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione-azacyclohexane-C-piperazine-CO is a synthesized E3 ligase ligand-linker conjugate that can be used to synthesize PROTAC LRRK2 Degrader-4. PROTAC LRRK2 Degrader-4 is a potent LRRK2 PROTAC degrader with anti-neuroinflammatory activity.

4'-Acetyl-chrysomycin A is an analog of chrysomycin A. 4'-Acetyl-chrysomycin A has antibacterial activity.

L-759656 is a selective cannabinoid CB2 receptor agonist, with the Ki of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC50 of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.

(±)-WB 4101 is a highly selective α1-adrenergic receptor antagonist. (±)-WB 4101 blocks norepinephrine-induced vascular smooth muscle contraction to exert antihypertensive and benign prostatic hyperplasia (BPH)-relieving effects. (±)-WB 4101 is promising for research of hypertension and BPH.

PSEC13 is an activator of HSF-1/DAF-16 axis. PSEC13 can upregulate heat shock proteins. PSEC13 can form hydrogen bonds with key residues in the HSP-16.2 active site. PSEC13 can be used to enhance proteostasis and extend lifespan through the modulation of HSP-16.2. PSEC13 could promote the nuclear translocation of daf-16, upgrading the proportion of intermediate. PSEC13 can be studied in research for aging and age-related diseases.

F-14258 is a 5-HT1B/1D receptor agonist. F-14258 can achieve receptor specific analgesia through local administration. F-14258 can be used for research on ear pain.

AR-DBD ligand-1 is an AR-DBD ligand. AR-DBD ligand-1 can be used to synthesize PROTAC LYA914.

AR-DBD ligand-Linker Conjugate 1 is a conjugate of AR-DBD ligand and linker. AR-DBD ligand-Linker Conjugate 1 can be used to synthesize PROTAC LYA914.

PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.

TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression).