HDAC6 ligand-linker conjugate 1 is a conjugate of HDAC6 ligand and linker, which can be used to synthesize PROTACs such as PROTAC HDAC6 degrader 5.

Zidapamide (Compound 4a) is an isomer of indapamide. Zidapamide has diuretic and natriuretic activities. Zidapamide is used in the study of hypertension.

Ad-JQ1 (Compound 16) is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 and a PROTAC linker, which recruits E3 ligases. Ad-JQ1 can be used for synthesis of PROTAC β-NF-JQ1

KHS108-MV1 is a conjugate of KHS108 and MV1. KHS108 is a ligand for TACC3. MV1 is an IAP antagonist that binds to cIAP1, cIAP2, and XIAP. KHS108-MV1 can be used in the research of breast cancer and fibrosarcoma.

T26A is a competitive prostaglandin transporter (PGT) inhibitor (Ki=378 nM). T26A is promising for research of prostaglandin signaling and inflammatory diseases (e.g., glaucoma, pulmonary hypertension) .

OPC-33540 is a highly selective and competitive PDE3 inhibitor with IC50 values of 0.32 nM (PDE3A) and 1.5 nM (PDE3B). OPC-33540 exhibits IC50s against PDE1, PDE2, PDE4, PDE5, and PDE7 of 42.9, 52.3, 100.8, 2.5, and 51.3 μM, respectively. OPC-33540 significantly enhances cAMP accumulation in platelets and effectively inhibits thrombin-induced platelet aggregation. OPC-33540 can be used in antithrombotic studies.

BMS-317180 is an orally active and potent growth hormone secretagogue receptor (GHS-R) agonist (EC50=7.9 nM). BMS-317180 stimulates endogenous growth hormone (GH) release. BMS-317180 is promising for research of age-related frailty, osteoporosis, and cancer cachexia.

AVE-5997 is a selective b>D3 antagonist. AVE-5997 antagonizes MK-801)-induced hyperactivity. AVE-5997 can be used in the research of schizophrenia.

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.

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.

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.

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.

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.