BQ-610 is a selective antagonist of the endothelin A receptor (ETA receptor). BQ-610 specifically blocks the ETA receptor, competitively inhibiting the binding of endothelin-1 (ET-1) (a vasoconstrictive peptide) to the receptor, thereby blocking the effects of ET-1 such as vascular smooth muscle contraction, cell mitosis, and inhibition of hormone secretion. BQ-610 significantly alleviates cerebral vasospasm in rabbits. BQ-610 blocks the bronchial epithelial and pulmonary vascular cell proliferation caused by cigarette smoke in rat models. BQ-610 can delay the natural luteal regression in the cow's uterus. BQ-610 can be used for research on vasospasm, abnormal cell proliferation, and reproductive endocrine disorders.

NGD 94-1 (dimaleate) is a potent and selective dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research[1][2].

BMS-505130 (fumarate) is a potent, selective and orally active serotonin transport inhibitor with a Ki for binding to the serotonin transporter of 0.18 nM (Ki for norepinephrine and dopamine transporters of 4.6 and 2.1 μM, respectively). BMS-505130 (fumarate) can be used for the research of neurological disease, such as depression.

UNC7437 is a inositol phosphate multikinase (IPMK) inhibitor, with an IC50 value of 26.2 nM. UNC7437 exhibits anti-proliferative activity against glioblastoma cells. UNC7437 decreases the accumulation of InsP4, InsP5, and InsP6 in cells. UNC7437 can be used for the study of TEN-negative glioblastoma models.

BRL-26830A is a β-adrenergic receptor agonist. In obese mouse models, BRL-26830A reduces body weight and increases metabolic rate. BRL-26830A stimulates insulin release and significantly reduces blood glucose levels in ICR mouse models. BRL-26830A can be used to study endocrine and metabolic diseases such as obesity and diabetes.

KW-5092 (fumarete) is a gastrokinetic agent. KW-5092 (fumarete) can increase intraluminal 5-HT release via the stimulation of cholinergic neurons .

9-cis-UAB30 is a rexinoid agonist. 9-cis-UAB30 significantly decreases the proliferation, viability, and motility of both patient-derived xenografts (PDXs). 9-cis-UAB30 induced cell-cycle arrest as demonstrated by the significant increase in the percentage of cells in G1 and a decrease in the percentage of cells in S phase by downregulating SKP2 and/or 20S proteasome activity, which leads to increased p27kip1 protein stability. 9-cis-UAB30 downregulates the abundance of stem cell marker mRNAs (Oct4, Nanog, Sox2, nestin) and upregulates the abundance of differentiation marker mRNAs (β3-tubulin, NSE, HOXC9, GAP43). 9-cis-UAB30 has no adverse effects on the central nervous system and cardiovascular system at the tested dose. 9-cis-UAB30 can be used for the study of neuroblastoma, cutaneous T-cell lymphomas, and breast cancer.

BCN-HS-PEG2-VA-PABC is a ADC linker that can be used in the synthesis of PL1601.

PZ671 is a potent Bcl-xL PROTAC degrader with an IC50 of 1.3 nM (MOLT-4 cells) and a DC50 of 0.9 nM (Bcl-xL). PZ671 induces apoptosis in MOLT-4 cells. PZ671 effectively inhibits tumor growth and rapidly reverses transient platelet counts reduction in MOLT-4 xenograft mice. PZ671 can be used for the research of cancer, such as small cell lung cancer (SCLC).

BCL-xL ligand 2 is a ligand for BCL-xL. BCL-xL ligand 2 can be conjugated with E3 ligase Ligand and linker to synthesize Bcl-xL PROTAC degrader PZ671.

Bay-y-1015 is an orally active quinoline-based 5-lipoxygenase inhibitor. Bay-y-1015 inhibits LTB4 and LTC4 synthesis. Bay-y-1015 can be used in the research of inflammatory diseases.

PD-254552 is a MEK inhibitor. PD-254552 exhibits hepatotoxicity and gastrointestinal toxicity in mice.

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.