Mps1/TTK-IN-1 (Compound cpd-5), a derivative of NMS-P715, is a Mps1 kinase inhibitor with an IC50 of 9.2 nM and a Kd of 1.6 nM. Mps1/TTK-IN-1 specifically targets the ATP-binding pocket of the Mps1 kinase. Mps1/TTK-IN-1 maintains inhibitory activity against Mps1 drug-resistant mutants (C604Y, C604W) with IC50 values of 170 and 19 nM and Kd values of 471 and 349 nM. Mps1/TTK-IN-1 can block the phosphorylation of kinetochore protein KNL1 mediated by Mps1, interfere with the spindle assembly checkpoint function, prevent the correct separation of chromosomes, and thereby inhibit the mitosis and proliferation of tumor cells.

MMP-9-IN-13 (Example 1) is a selective inhibitor of human MMP9 with an IC50 value of 0.02 nM. MMP-9-IN-13 can be used in the research of ocular surface.

Man-GIcNAc-oxazoline (compound 6) is an N-acetylglucosamine (GlcNAc) and azide-modified disaccharide that can be used to label antibodies. Man-GIcNAc-oxazoline can be synthesized as an ADC via click chemistry.

LUF7996 is a CCR2 PROTAC Degrader degrading CCR2 with DC50 = 2.6 μM. LUF7996 demonstrates engagement of both and the E3 ligase cereblon and displays sustain and concentration-dependent degradation of CCR2. LUF7996 reliance on the lysosomal pathway to induce CCR2 degradation. LUF7996 efficiently inhibits monocyte migration in virto. (Pink: CCR2 ligand ; Blue: Cereblon ligand ; Black: linker).

Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

Largazole thiol, the active form of Largazole, is a potent, selective and brain-penetrant class I HDAC inhibitor. Largazole thiol. Largazole thiol exerts antitumor and neuroprotective effects. Largazole thiol can be used for research of Glioblastoma.

IDH1 ligand 1 (Compound 18) can serve as a negative control for the IDH1 target, with no detectable affinity for wild-type IDH1 and an IC50 >10,000 nM.

HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis.

GSPT2 degrader-1 (compound 619) is a selective molecular glue GSPT2 degrader targeting GSPT2. GSPT2 degrader-1 contains Thalidomide and the linker of MDEG-541. GSPT2 degrader-1 induces the degradation, but not GSPT1 or myelocytomatosis oncogene (MYC). GSPT2 degrader-1 can be used for research of gastrointestinal cancer.

GSK190937 is a type II platelet-derived growth factor receptor alpha (PDGFRA) human kinase inhibitor with antimalarial activity. GSK190937 can inhibit the formation of hemozoin in the malaria parasite, resulting in the accumulation of free hemoglobin within the malaria parasite. GSK190937 shows IC50 values of 0.22, 0.59 and 0.25 μM against P. falciparum NF54, K1 and Dd2 parasite. GSK190937 shows an IC50 of 25 μM for CHO cells. GSK190937 can be used for research of malaria.

GIT1-IN-1 is an inhibitor of ARF GTPase-activating protein 1 (GIT1) with a KD of 6.2 μM. GIT1-IN-1 induces apoptosis (apoptosis) in liver and colon cancer cells, arrests the cell cycle at the G2/M phase, and inhibits cell proliferation, colony formation and migration. GIT1-IN-1 inhibits the activities of MEK and ERK, reduces the expression level of cyclin D1, and stabilizes cyclin B1 protein in liver and colon cancer cells. GIT1-IN-1 can be used in the research of liver cancer and colon cancer.

FXR agonist 16 is a FXR agonist with an EC50 of 2.2 μM. FXR agonist 16 activates FXR transcriptional activity, upregulates SHP and BSEP, and downregulates Cyp7a1. FXR agonist 16 exhibits hepatoprotective activity and reduces AST and ALT levels in free fatty acid-induced hepatocellular injury models. FXR agonist 16 can be used for the research of liver injury.

Feruloyl-CoA (Feruloyl-coenzyme A) is a cinnamoyl-CoA ester substrate involved in the biosynthesis of lignin and coumarin in plants. Feruloyl-CoA acts as a substrate for cinnamoyl-CoA reductase 1-dependent reduction reaction with NADPH to produce cinnamaldehyde. Feruloyl-CoA is a precursor that generates Scopoletin via spontaneous trans/cis isomerization and lactonization of its side chain.

FBPase-IN-6 (Compound 96) is an orally active FBPase inhibitor with an IC50 value of 1.769 μM. FBPase-IN-6 modulates AMPK/mTORC1/S6K signaling pathways. FBPase-IN-6 improves glucose tolerance, enhances insulin sensitivity, and promotes insulin secretion in type 2 diabetic mice.

Farabursen (RGLS8429; RG1015) is a blood-brain barrier-permeable miR-17 inhibitor. Farabursen derepresses Pkd1 and Pkd2, the target genes of miR-17, increases the levels of PC1 and PC2, and reduces cyst growth. Farabursen decreases renal cyst growth, kidney weight-to-body weight ratio, cyst index, proliferation index, and blood urea nitrogen levels in mouse models. Farabursen is applicable to research related to autosomal dominant polycystic kidney disease.

Dotarizine is a novel Piperazine derivative and antimigraine agent. Dotarizine exhibits Ca2+ channel blocking properties. Dotarizine decreases the release of lactate dehydrogenase. Dotarizine shows 5-HT receptor blocking effect.

DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor with a target pIC50 of 4.801. DM245 activates EPAC1 to increase Rap1-GTP levels, with no activation of EPAC2 or PKA. DM245 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM245 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing αSMA and Collagen I levels. DM245 exhibits minimal cytotoxicity in normal human lung fibroblasts, with negligible loss of intact nuclei after 72 h exposure.

DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells, with no activation of EPAC2 or PKA. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts.

DM-1157 is an orally active asymmetric bisquinoline heme inhibitor with a IC50 of 1.6 μM and a Kd of 1.7 μM. DM-1157 binds to heme dimers in solution, inhibits β-hematin formation, suppresses hemozoin formation in the digestive vacuole of Plasmodium falciparum, accumulates in the digestive vacuole of Plasmodium falciparum, induces enlargement of the digestive vacuole of Plasmodium falciparum, and inhibits the growth of Chloroquine-sensitive and resistant Plasmodium falciparum strains. DM-1157 can be used for the research of malaria and Plasmodium falciparum-type malaria.

Dimefluthrin is an insecticide. Dimefluthrin exhibits contact toxicity against large red imported fire ant workers. Dimefluthrin undergoes horizontal transfer among red imported fire ant workers, causing secondary mortality in recipient workers. Dimefluthrin is a neurodevelopmental toxicant, which can reduces acetylcholinesterase activity, impairing neurotransmitter.

Diethyl benzylmalonate is a drug intermediate that can be used for the synthesis of central inhibitory agents.

Desmethylcitalopram hydrobromide (DCIT hydrobromide) is a drug impurity.

DdBIC is a pyroptosis inducer. DdBIC binds to Nur77 and triggers its translocation to mitochondria, activates SDHA to deplete succinyl-CoA, disrupts heme homeostasis, induces electron leakage, and elicits mitochondrial ROS production. DdBIC induces mitochondrial ROS that oxidatively activates OMA1, promotes OPA1 cleavage and its release into the cytoplasm, activates the integrated stress response via PERK, and ultimately activates granzyme B to cleave GSDMC. DdBIC can be used for the study of melanoma.

COX-2/CaV2.2-IN-1 is an orally active and selective dual COX-2/CaV2.2 inhibitor, exhibiting a COX-2 IC50 of 0.26 μM and a CaV2.2 IC50 of 0.29 μM. COX-2/CaV2.2-IN-1 suppresses inflammatory responses and inflammatory mediator (IL-6, TNF-α, NO) production. COX-2/CaV2.2-IN-1 produces pronounced analgesic effects in diverse models of inflammatory, neuropathic, and visceral pain. COX-2/CaV2.2-IN-1 can be used for the research of chronic pain.

CGP-45688 is an orally active non-steroidal aromatase inhibitor with an ED50 of 30-100 μg/kg. CGP-45688 can reduce the level of estrogen in the body, thereby inhibiting the growth of estrogen-dependent tumors. CGP-45688 inhibits the growth of estrogen-dependent breast tumors in rat models. CGP-45688 disrupts the ovarian cycle and inhibits the weight of the uterus. CGP-45688 can be used for the study of breast cancer.

CDK9-IN-48 is a CDK9 inhibitor with an IC50 of 1.37 nM. CDK9-IN-48 inhibits the proliferation of various cancer cells. CDK9-IN-48 can be used in the research of cancers such as acute myeloid leukemia and prostate cancer.

CC-M-1 is a potent and selective PI3K/mTOR inhibitor. CC-M-1 inhibits PI3Kα/β/γ/δ and mTOR with IC50 values of 0.68, 1.02, 1.03, 8.03, and 15 nM, respectively. CC-M-1 inhibits the proliferation of colorectal cancer cell lines, including HCT-116 (IC50 = 0.38 μM) and HT-29 (IC50 = 1.70 μM). CC-M-1 can be used for colorectal cancer (CRC) research.

CCL17-IN-1 (Compound Ex.132) is a CCL17 secretion inhibitor with an EC50 of 0.2 nM. CCL17-IN-1 can be used in the research of autoimmune diseases, dermatological conditions, and respiratory disorders.

BXY-14 is a TLR2 agonist and vaccine adjuvant. BXY-14 significantly downregulates the expression of intratumoral PD-L1 in mouse models. BXY-14 acts as a vaccine adjuvant to induce antibody responses. BXY-14 exhibits synergistic efficacy when combined with the anti-PD-L1 monoclonal antibody Atezolizumab in mouse models of melanoma, and prolongs overall survival. BXY-14 is applicable to research related to melanoma.

BL-1021 is an orally active ion channel blocker. BL-1021 significantly reduces symptoms of neuropathic pain without noticeable sedation or cardiac arrhythmias. BL-1021 can be used in the research of acute and chronic pain.