PySAHA is a multifunctional HDAC inhibitor. PySAHA can degrade intracellular HDAC via a hydrophobic tagging mechanism. PySAHA also possesses photodynamic therapeutic activity and can generate reactive oxygen species under light irradiation. PySAHA can inhibit the proliferation, migration and induce cell apoptosis of breast cancer cells. PySAHA has antitumor activity and can be used in breast cancer research.

WMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2].

MPT0G413 (Compound 6) is a potent, selective, orally active and brain-penetrant HDAC6 inhibitor with an IC50 of 3.92 nM. MPT0G413 decreases not only the level of phosphorylation of tau proteins but also the aggregation of tau proteins. MPT0G413 can ameliorate the impaired learning and memory. MPT0G413 can be used for the research of neurological disease, such as Alzheimer's disease.

HDAC6 ligand-5 is a binding ligand of HDAC6 and can be used to synthesize PROTACs such as PROTAC HDAC6 degrader 5.

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.

DBCO-PEG8-VKG-CPT2 is a drug-linker conjugate for ADC. DBCO-PEG8-VKG-CPT2 consists of a topoisomerase 1 inhibitor (7-MAD-MDCPT) and a stable and cleavable linker (DBCO-PEG8-VKG). DBCO-PEG8-VKG-CPT2 can be used for synthesis of ADCs.

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) .

Adamantan-C-amide-PEG2-C2-amine (Compound 8) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC β-NF-JQ1.

Pomalidomide-C2-PEG-NHCO-C2-COOH is a conjugate of the CRBN ligand and the linker (E3 Ligase Ligand-Linker Conjugate). Pomalidomide-C2-PEG-NHCO-C2-COOH can be used for synthesizing PROTAC ASK1 degrader dASK1.

dASK1 is a selective and cereblon (CRBN)-based PROTAC degrader of apoptosis signal-regulating kinase 1 (ASK1). dASK1 forms a stable ternary complex with ASK1, facilitating ASK1 rapid and sustained degradation via the ubiquitin-proteasome pathway. dASK1 demonstrates potent ASK1 degradation. dASK1 can be used for the research of steatohepatitis.

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.

LD-110 is a highly efficient and effective PROTAC degrader targeting LSD1 (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 can be used for the study of esophagus squamous cancer.

LAG-3 PROTAC-1 is a potent LAG-3 PROTAC degrader with a DC50 of 0.27 μM. LAG-3 PROTAC-1 can be used in cancer immunology research.

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.

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.