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.

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.

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.

PWT-33597 (VDC-597) is a dual inhibitor of PI3Kα and mTOR, which can effectively block the signaling downstream of PI3K and mTOR. PWT-33597 is capable of inducing tumor cell apoptosis and inhibiting tumor growth. PWT-33597 has anti-tumor activity and can be used in the research of tumors such as renal cell carcinoma.

PWT-33597 (VDC-597) free base is a dual inhibitor of PI3Kα and mTOR, which can effectively block the signaling downstream of PI3K and mTOR. PWT-33597 free base is capable of inducing tumor cell apoptosis and inhibiting tumor growth. PWT-33597 free base has anti-tumor activity and can be used in the research of tumors such as renal cell carcinoma.

GaSal-2 is a water-soluble anti-pseudomonal agent that targets the extracellular hemocyte HasAp. It binds tightly to HasAp, blocks the transcriptional activation of the bacterial cell surface signaling cascade, and inhibits the growth of Pseudomonas aeruginosa.

(E/Z)-MitoTam (iodide, hydriodide) (MitoTam (iodide, hydriodide)) is the E/Z mixture of MitoTam iodide, hydriodide. MitoTam iodide, hydriodide is a Tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells. MitoTam iodide, hydriodide causes apoptosis.

SKLB06329 is a potent selective Type I PRMTs inhibitor. SKLB06329 shows good selectivity for PRMT6 (IC50 = 3.86 nM) over Type II/III PRMTs (PRMT5/7) and shows no significant inhibition against various lysine methyltransferases (PKMTs). SKLB06329 significantly inhibits the proliferation of triple-negative breast cancer (TNBC) cells, induces apoptosis, and suppresses the expression of asymmetric dimethylarginine (ADMA) within cells. SKLB06329 can be used for triple-negative breast cancer research.

Envometinib (Compound B) is a dual-MEK inhibitor that works through Deep Cyclic Inhibition (DCI). Envometinib has antitumor activity in various in vivo models. Envometinib can be studied in RAS and RAF mutated cancer such as colorectal cancer and melanoma.

PD 128483 is a selective dopamine autoreceptor agonist. PD 128483 can be used for the research of neurological disease.

BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL).

AR493 is an autophagy activator acting on AMPK (adenosine monophosphate-activated protein kinase). AR493 regulates pathways related to cellular energy sensing and increases autophagy levels. AR493 is promising for research of aging-associated diseases (such as diabetes, neurodegenerative diseases) and autophagy regulation.

CZL-S092 is a PLK4 inhibitor with an IC50 value of 0.9 nM and excellent selectivity over other PLK4 family members (PLK1, PLK2, and PLK3). CZL-S092 exhibits anti-neuroblastoma activity in vitro (IMR-32 cells, IC50 = 1.143 μM). CZL-S092 inhibits cell migration and halts the cell cycle and induces apoptosis. CZL-S092 can be used in studies of various cancers including neuroblastoma cancer.

DF 1111301 is a new antiallergic compound endowed of antihistamine-H1 and anti-PAF activities.

NBI-75043 is an antagonist of H1 receptor.

CHNQD-01269, a brefeldin A-cinnamate derivative, is an Arf1 inhibitor. CHNQD-01269 exhibits potent cytotoxic activity against HepG2 and BEL-7402 cells, with IC50 values of 0.29 and 0.84 μM, respectively. CHNQD-01269 is indicated for hepatocellular carcinoma (HCC) research.

CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8. CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing.

Suvigletistat (compound 2) is a potent transglutaminase 2 (TG2) inhibitor with an IC50 value of ＜0.5 µM.

JNJ-79883960 is a NLRP3 inhibitor. JNJ-79883960 can be used for the study of inflammation.

WRN inhibitor 19 (Compound 40) is a WRN helicase inhibitor (IC50: 3.7 nM). WRN inhibitor 19 exhibits selective antiproliferative activity in WRN-dependent cancer cells. WRN inhibitor 19 inhibits WRN helicase function by competitively binding to the ATP site and induces DNA damage and cell cycle arrest. WRN inhibitor 19 can be used in the study of WRN-dependent cancers.

1-Naphthyl U-47700 is an α-isomer. 1-Naphthyl U-47700 is a racemic mixtures of the trans-isomers [R,R and S,S]. 1-Naphthyl U-47700 activates MOR in a concentration-dependent manner (EC50 > 23 μM).

RN277 is an inhibitor for LRRK2 type II kinase. RN277 can be used as a cellular tool targeting the LRRK2 inactive state. RN277 can inhibit LRRK1 kinase activity in vitro. RN277 inhibits LRRK2 kinase activity in vitro (IC50 = 70 nM). RN277 reduces phosphorylation of Rab8a dose-dependently. RN277 can be studied in research for Parkingson’s disease.