GW-300 is a SREBP cleavage-activating protein (SCAP) ligand that can be used for the study of endocrinology and metabolic disease.

A-350619 is a novel sGC activator. A-350619 increases intracellular cGMP levels. A-350619 significantly induces penile erection.

WRN inhibitor 20 (Compound 14c) is a WRN degradation agent. WRN inhibitor 20 exhibits strong degradation activity in various cells, such as HCT-116 (DC50 = 1.7 µM), SW-48 (DC50 = 3.0 µM), and SW-480 (DC50 = 5.9 µM) cells. WRN inhibitor 20 exhibits potent anti proliferative, pro apoptotic, migration inhibiting, and DNA damage inducing effects in MSI-H cells. WRN inhibitor 20 can be used for research on cancer.

TM-04-064-02 is a molecular glue degrader. TM-04-064-02 induces proteins (such as IKZF1/3, PPIL4, ETF1 and PDE6D) to bind to CRBN, promoting their ubiquitination and degradation.

JWJ-01-378 is a selective TRK PROTAC degrader. JWJ-01-378 efficiently degrades WT TRK and TPM3-TRKA fusion proteins and inhibits downstream pERK signaling, while showing limited efficacy against TRK inhibitor resistant mutants and ALK fusions. JWJ-01-378 potently suppresses cancer cell proliferation.

dAurAB2 is a dual-degrading PROTAC that potently degrades Aurora-A and Aurora-B with DC50s of 59 nM and 39 nM, respectively. dAurAB2 reduces N-Myc levels in MYCN-amplified IMR32 neuroblastoma cells. dAurAB2 can be used for the study of neuroblastoma.

dAurAB5 is a dual Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma.

DOTA-ALB-02 is an albumin-bound FAP inhibitor (FAPI) ligand. DOTA-ALB-02 labeled with 177Lu has a high FAP-binding affinity and enhanced tumor uptake and retention with a significant tumor/nontarget ratio. DOTA-ALB-02 can be used for PET/CT and SPECT/CT imaging of cancers, especially late-stage cancers.

DOTA-ALB-01 is an albumin-bound FAP inhibitor (FAPI) ligand. DOTA-ALB-01 labeled with 68Ga or 177Lu has a high FAP-binding affinity and enhanced tumor uptake and retention. DOTA-ALB-01 can be used for PET/CT and SPECT/CT imaging of cancers, especially late-stage cancers.

NOTA-IMB-RGD is a dual molecular probe targeting integrin αvβ3 and programmed death ligand-1 (PD-L1). NOTA-IMB-RGD blocks the PD-1/PD-L1 signaling pathway and integrin αvβ3-overexpressing tumor vasculature. NOTA-IMB-RGD is promising for research of solid tumors co-expressing PD-L1 and αvβ3 (e.g., glioma, breast cancer).

SA-13353 is a TRPV1 agonist with cardioprotective effect. SA-13353 can be used for the research of cardiovascular disease .

RGD-DA6 is an αvβ3-targeted ligand. RGD-DA6 consists of RGDfK (an integrin αvβ3-targeted RGD peptide), DOTADG, d-Glu, Lys, AMBA, and IPBA. RGD-DA6 can be radiolabeled as an αvβ3-targeted radioligand and used for high-contrast tumor imaging and enhanced anticancer efficacy.

SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer.

sEH-H ligand 2 is an sEH inhibitor and a ligand for the target protein for PROTAC (sEH). sEH-H ligand 2 can be used to synthesize PROTAC sEH-degrader-4.

POI ligand-2-NH-C10H20-NH-Boc is a target protein ligand linker conjugate that contains a GPX4 ligand and a PROTAC linker), which can recruit E3 ligases. POI ligand-2-NH-C10H20-NH-Boc can be used for synthesis of PROTAC GPX4 degrader-5

CJ-15161 is a κ-opioid receptor agonist. CJ-15161 can be used to study physiological functions such as pain relief and emotional regulation.

GAP-1173149 is a Chikungunya Virus polymerase inhibitor targeting the CHIKV nsP4 RNA-dependent RNA polymerase.

Y-99 is a PORCN inhibitor with an IC50 of 155.4 nM against the Wnt/β-catenin signaling pathway. Y-99 inhibits the expression of p-LRP6, β-catenin, and c-Myc.

ADT-1004 is an inhibitor of RAS. ADT-1004 can be studied in research for Ras-mediated diseases.

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.