WR 151327 is an orally active radiation and chemoprotection protector. WR 151327 can suppress expression of HIV. WR 151327 can be used for the researches of infection and cancer.

Daledalin (UK 3557) is an orally active indoline antidepressant targeting noradrenaline and serotonin transporters in the brain. Daledalin enhances central monoaminergic neurotransmission to alleviate depressive symptoms. Daledalin is proming for rasearch of depression, including endogenous and neurotic depression.

Rivanicline (RJR-2403) hydrochloride is a neuronal nicotinic receptor agonist. Rivanicline hydrochloride is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hydrochloride can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hydrochloride can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).

TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain.

(E/Z)-Rivanicline ((E/Z)-RJR-2403, (E/Z)-Metanicotine) is the E/Z mixture of Rivanicline). Rivanicline is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype, Ki is 26 nM, which is more than 1000 times more inhibitory than α7 receptor.

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.