TBK1 ligand 2 (Compound 1b) is a TBK1 inhibitor. TBK1 ligand 2 can be used for synthesis of PROTAC TBK1 degrader-2.

MCC-AAQ-Exa is a drug-linker conjugates for ADC, obtained by condensing the linker with Exatecan and can be used to prepare antibody-drug conjugates (ADCs). MCC is an ADC linker containing a maleimide fragment.

(Rac)-TUL01101 (Compound I) is a selective JAK kinase inhibitor. (Rac)-TUL01101 can be used in the research of various diseases such as rheumatoid arthritis, atopic dermatitis, and alopecia areata.

YM-50001 is a potent and selective dopamine D4 receptor antagonist with a Ki 5.62 nM. YM-50001 can be used for the research of neurological disease .

FCE-20696 (hydrochloride) is an orally active immunomodulator. FCE-20696 (hydrochloride) also shows anti-inflammation and anti-infection effects. FCE-20696 (hydrochloride) can be used for the researches of infection, inflammation and immunology, such as adjuvant arthritis.

RS-86 is a potent, central acting, and selective muscarinic acetylcholine receptor agonist. RS-86 exhibits typical cholinergic excitatory effects, such as inducing smooth muscle contraction, ganglion depolarization, central hypothermia, etc. RS-86 can be used for research on Alzheimer's disease.

SQ 26490 is an active corticoid, moderate-potency edema formation inhibitor. SQ 26490 inhibits edema formation in rats.

PY-PAP is a photoactivatable affinity probe and a derivative of PY-60). PY-PAP retains the cellular function of activating YAP transcriptional activity. In 293A cells, PY-PAP can label cathepsin D (CTSD) and annexin A2 (ANXA2) through ultraviolet crosslinking and click reactions. PY-PAP plays a key role in identifying ANXA2 as the specific target of PY-60.

MU876 (Compound 32) is a MUS81 inhibitor with an IC50 of 0.5  μM. MU876 effectively inhibits MUS81-dependent homologous recombination (HR) and break-induced replication (BIR) pathways. MU876 sensitizes cancer cells to DNA-damaging agents, such as Cisplatin, through impairing their ability to repair DNA lesions. MU876 can be used for cancers chemotherapy research.

BLX-2477 is a potent and selective 15-lipoxygenase-1 (15-LOX-1) inhibitor with an IC50 value of 99 nM. BLX-2477 can inhibit the generation of inflammatory lipid mediators such as 15-hydroxy-eicosatetraenoic acid (15-HETE). BLX-2477 can be used for the research of inflammation and immunology.

Rimonabant carboxylic acid is a Ligand for Target Protein for PROTAC. Rimonabant carboxylic acid can be used to synthesize PROTAC CB1R Degrader-1.

SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders.

Midobrutinib (Example 13) is a BTK inhibitor (IC50: 0.813 nM). Midobrutinib can be used for research of diseases involving BTK, particularly cancer.

GT-02216 can bind to GCase allosterically and enhance its activity. GT-02216 enhances the activity of GCase in primary human fibroblasts dose-dependently reduces the accumulation of its substrate, hexosylsphingosine (HexCer). GT-02216 reduces the Tau accumulation in mutant GBA1 fibroblasts. GT-02216 can be used for the study of Parkinson’s disease.

NVP-QBE170 is a selective Epithelial sodium channel (ENaC) inhibitor with an IC50 of 57.5 nM. NVP-QBE170 potently inhibits ENaC function in HBECs and shows a longer duration of action. NVP-QBE170 significantly attenuates ENaC activity in the airways of guinea pig models. NVP-QBE170 can be used for hyperkalaemia research.

SMU-V18 is a vesicular stomatitis virus (VSV) inhibitor, with an EC50 of 6.2 μM. SMU-V18 inhibits VSV-GFP fluorescence intensity, viral mRNA/protein expression, and progeny virus replication. SMU-V18 interferes with early viral infection stages, also effective against wild-type VSV (VSV-WT). SMU-V18 inhibits VSV-GFP in mouse tissues and prolongs survival. SMU-V18 can be used for the study of vesicular stomatitis virus (VSV) infection.

ML210-ansaFc (Compound III-13) is a covalent GPX4 inhibitor with a [3]-ferrocenophane group (IC50 of 3.4 μM). ML210-ansaFc potently induces ferroptosis by increasing the level of ROSand promoting lipid peroxidation (LPO) in cancers cells. ML210-ansaFc has an anticancer activity and suppresses tumor growth in tumor 3D spheroids. ML210-ansaFc can be used for cancer therapy resistance research.

BRAF ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate that can be used to synthesize PROTAC CST905.

SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction.

VS1150 (Compound 11) is a BCR-ABL-targeting phosphorylation-inducing chimeric small molecule (PHICS). VS1150 significantly inhibits oncogenic kinase BCR-ABL signaling by inducing inhibitory phosphorylation at its Y253 (EC50: 69 nM), subsequently triggering cell apoptosis. VS1150 also inhibits other oncogenic ABL fusions and drug-resistant mutants like T315I. VS1150 can be used for chronic myeloid leukemia (CML) and other ABL fusion-driven cancers research.

SJ11646 is a Dasatinib-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model.

N-Deshydroxyethyl Dasatinib-C3-NH2 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for LCK and a PROTAC linker, which recruits E3 ligases. N-Deshydroxyethyl Dasatinib-C3-NH2 can be used for synthesis of PROTAC SJ11646

CP-74667 is a quinolone antibacterial agent. CP-74667 shows high activity against Xanthomonas maltophilia (MIC50 = 1 μg/mL), Staphylococcus spp. (MIC50 = 0.06-0.12 μg/mL) and enterococci (MIC50 = 0.5-4 μg/mL).

E 5065 is an orally active antibacterial agent. E 5065 exhibits potent in vitro activity against Gram-negative microorganisms, Gram-positive cocci, and anaerobes. E 5065 exhibits an MIC90 of 0.5 μg/mL against Clostridium spp. E 5065 provides protection against experimental infections caused by P. aeruginosa.

PS21M is a negative control of CPS-021. PS21M cannot effectively degrade PAK4 in MDA-MB-231 cells.

PNU-183792, a 4-oxo-dihydroquinoline, is an orally active HSV polymerases inhibitor. PNU-183792 shows a broad-spectrum antiviral activity, with IC50 values of 0.69 μM, 0.37 μM and 0.58 μM for human cytomegalovirus (HCM), varicella zoster virus and HSV polymerases, respectively. PNU-183792 is inactive against human α, γ and δ polymerases. PNU-183792 also inhibits simian varicella virus (SVV), murine cytomegalovirus (MCMV) and rat cytomegalovirus (RCMV).

LO-3-63, a Ribociclib analog bearing a truncated fumaramide handle, is a PROTAC-like CDK4/6 degrader. LO-3-63 induces CUL4DCAF16-dependent degradation of CDK4/6 in cells.

KWZY-11 (Compound 11) is a potent PARP/CDK6 dual inhibitor with IC50 values of 156.8, 197.3, and 13.3 nM for PARP1, PARP2, and CDK6, respectively. KWZY-11 inhibits tumor cell proliferation by regulating the Wnt/β-catenin signaling pathway. KWZY-11 induces excessive DNA damage and apoptosis in MDA-MB-231 breast cancer cells.

Imitrodast sodium is an inhibitor of thromboxane synthase. Imitrodast sodium can be used in the research of bronchoconstriction.

STAT6 ligand-1 is a ligand for STAT6. STAT6 ligand-1 can be used for synthesizing PROTACs such as STAT6 degrader-2.