IKZF1/3 ligand-1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC IKZF1/3 Degrader-1. PROTAC IKZF1/3 Degrader-1 is a potent IKZF1/3 PROTAC degrader with neuroprotective activity.

BCL6 ligand-5 (Compound 37) is a BCL6 ligand. BCL6 ligand-5 can be used as a ligand for target protein for PROTAC to develop and design degraders for PROTAC BCL6, such as PROTAC BCL6 Degrader-2. BCL6 ligand-5 can also be used in tumor research.

DEL1187-126-28-16 is a JAK3 inhibitor with IC50s of 10 and 0.97 nM against JAK3 WT in 0 and 60 min. DEL1187-126-28-16 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-28-16 can be used for the study of immune-mediated diseases.

CLT-28643 is an integrin α5β1 inhibitor. CLT-28643 can inhibit the high expression of integrin α5β1 in the bleb at early time-points after surgery and promote wound healing process.

DNDI-6510 (Compound (S)-x38) is a non-covalent SARS-CoV-2 MPro inhibitor with a IC50 of 0.04 μM. DNDI-6510 has a potent antiviral activity across SARS-CoV-2 and its variants as well as a weak efficacy to SARS-CoV-1. DNDI-6510 significantly improves drug exposure in metabolically humanized mice model (8HUM).

TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.

INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.

MW073 is a highly selective and orally active 5-HT2BR antagonist (IC50 =70 nM). MW073 exerts its effects by concentration-dependently inhibiting receptor activity and β-arrestin-1 recruitment. MW073 ameliorates synaptic plasticity and behavioral deficits, including aggression, in Alzheimer’s disease (AD) mouse models. MW073 can be used for Alzheimer’s disease (AD) research[1][2].

VU0494372 is an activator of potassium ion channel KCNQ1. VU0494372 can significantly enhance the cell surface expression and transport efficiency of KCNQ1. VU0494372 does not alter KCNQ1 mRNA levels and protein degradation rate, and has no significant cytotoxicity. VU0494372 can be used for research on cardiovascular conditions.

RB-90740 is a type of biological reducing agent. RB-90740 is activated through metabolic reduction and generates cytotoxic products, thereby selectively killing tumor cells (usually in a hypoxic environment). RB-90740 has selective toxicity towards hypoxic cells, which is mainly achieved by causing DNA strand breaks and activating reducing enzymes (such as Cytochrome P450). RB-90740 does not initially exhibit cytotoxicity similar to its in vitro properties in hypoxic cells in mouse models. RB-90740 can be used to study the tumor physiological environment

Elzasonan (CP-448187) is a 5-hydroxytryptamine1B receptor antagonist. Elzasonan is used in research on depression.

BTK/IKZF1/3 ligand 1 is a BTK/IKZF1/3 PROTAC ligand. BTK/IKZF1/3 ligand 1 can be conjugated with E3 ligase Ligand and linker to synthesize PROTAC BTK/IKZF1/3 Degrader-1. PROTAC BTK/IKZF1/3 Degrader-1 can be used for cancer research.

Zandelisib (ME-401) hydrochloride is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib hydrochloride can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib hydrochloride can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma.

Multi kinase ligand 4 is a target protein ligand used in the synthesis of PROTAC DB-0646.

ZINC000081009201 is a potent poly(ADP-ribose) polymerase 1 (PARP1) inhibitor with an IC50 value of 1.4767 μM. ZINC000081009201 is promising for research of triple-negative breast cancer (TNBC).

Dione-piperidine-indazol-piperazin-cyclohexyl-NH2 is an E3 ligase ligand-linker conjugate that incorporates a CRBN ligand and linker. Dione-piperidine-indazol-piperazin-cyclohexyl-NH2 can be used for synthesis of PROTAC MD-4251.

6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole is an E3 ligase ligand used in the synthesis of the PROTAC Androgen receptor degrader-1.

A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer.

DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies.

UCD0168 is a Serotonin transporter (SERT) inhibitor that acts as a full serotonin releasing agent (SRA). UCD0168 can be used for depression, addiction and post-traumatic stress disorder (PTSD) research.

NEU-5123 is a human kinase inhibitor with potent inhibitory activity to several kinases. NEU-5123 is a Trypanosome proliferation inhibitor. NEU-5123 can be used for the research of infection.

rel-Asenapine (rel-Org 5222) hydrochloride is a relative configuration of Asenapine hydrochloride. Asenapine (Org 5222) hydrochloride, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine hydrochloride can be used in the research of schizophrenia and bipolar disorder.

M6766 is a selective endoplasmic reticulum oxidoreductase 1α (ERO1α) inhibitor with an IC50 of 1.4 μM and a KD of 1.1 μM. M6766 also inhibits ERO1β with an IC50 of 7.2 μM. M6766 binds to the flavin adenine dinucleotide-binding pocket in ERO1α. M6766 inhibits granule secretion, αIIbβ3 integrin activation, Ca2+ mobilization, and platelet aggregation. M6766 can be used for the research of neurological disease, such as ischemic stroke.

E3 Ligase Ligand-linker Conjugate 195 is a conjugate of the CRBN ligand and the linker. E3 Ligase Ligand-linker Conjugate 195 can be used for synthesis of PROTACs such as APH02174.

UCD0820 is a Serotonin transporter (SERT) inhibitor that acts as a partial serotonin releasing agent (SRA). UCD0820 can be used for depression, addiction and post-traumatic stress disorder (PTSD) research.

Anisodine (Daturamine) is a neuroprotective compound that reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine inhibits calcium ion influx and reactive oxygen species (ROS)levels. Anisodine leads to decreased aspartate levels during hypoxia.

BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease.

XB2M54 is a selective XIAP antagonist. XB2M54 inhibits NOD2-mediated inflammatory signaling. XB2M54 is an E3 ligase ligand. XB2M54 can be used for synthesis of PROTAC ERα Degrader-1.

AMG-34 is a GCN2-targeting agent with IC50 values of 0.395 μM, 0.010 μM, 1.07 μM and ＞ 10 μM for GCN2, PERK, HRland PKR, respectively.

BRL-41992 is a selective α₂B-adrenergic receptor antagonist. BRL-41992 exhibits 94-fold higher selectivity for the α₂B-receptor than for the α₂A-receptor with Kᵢ values in neonatal rat lung tissue (expressing the α₂B-receptor) and in human platelet membranes (expressing the α₂A-receptor) of 1.1 and 103.3 nM. BRL-41992 can be used to verify the functional differences of α₂ receptor subtypes.