LCC03 is a salicylanilide derivative and autophagy inducer, dose-dependently suppresses proliferation and retarded cell-cycle progression in CRPC cells (IC50, 0.69 to 4.8 uM).The classical autophagy features, including autophagosome formation and LC3-II conversion, were dramatically shown in LCC03-treated CRPC cells, which was associated with the suppressed AKT/mTOR signaling pathways, a major negative regulator of autophagy.LCC03 also showed an expanded morphology of the endoplasmic reticulum (ER), increased expression of the ER stress markers GRP78 and PERK, and eIF2α phosphorylation.The PERK-eIF2α pathway contributed to the LCC03-induced autophagy.LCC03 suppressed the growth of CRPC xenografts in mouse bone without systemic toxicity in tumor-bearing mice.

MC-GGFG-DX8951 is a drug-linker conjugate for ADC with antitumor activity by using DX8951 (DNA topoisomerase I inhibitor), linked via the protease cleavable MC-GGFG linker.

MS 177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models.

MS910 (MS-910) is the first CRBN-recruiting MEK1/2 degrader (PROTC) with HT29 DC50 of 118/55 nM for MEK1/2 degradation, respectively.MS910 displays antiproliferation potency against HT29 cell with GI50 of 330 nM, degrade MEK1 and MEK2 and inhibit pERK signaling in a time-dependent manner.

MS934 (MS-934) is a VHL-recruiting MEK1/2 degrader (PROTAC) with HT29 DC50 of 18/9 nM for MEK1/2 degradation, respectively.MS934 is more potent at inhibiting the growth of HT-29, SK-MEL-28, H3122, and SUDHL1 cells. MS934 also displays good plasma exposure in mice.

MS9715 (MS-9715) is a NSD3-targeting PROTAC designed by linking BI-9321, a NSD3 antagonist, which binds NSD3's PWWP1 domain, with an E3 ligase VHL ligand.MS9715 achieves effective and specific targeting of NSD3 and associated cMyc node in tumor cells.MS9715 effectively suppresses growth of NSD3-dependent hematological cancer cells.MS 9715 effectively suppresses NSD3-and cMyc-associated gene expression programs, resembling effects of the CRISPR-Cas9-mediated knockout of NSD3.

QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls.QC-01–175 also rescued stress vulnerability in FTD neurons, phenocopying CRISPR-mediated MAPT-knockout.

RA306 (RA-306) is a selective, potent, orally active, ATP-competitive CaMKII inhibitor, inhibits CaMKII delta (IC50=15 nM), gamma (IC50=25 nM), and alpha (IC50=61 nM) isoforms.RA306 displays a good selectivity profile vs. kinases and non-kinase targets, as compared with KN-93.RA306 also displays a good cellular activity in cardiomyocytes from human, rat, and mice, with IC50s in the 200 nM range.Isoproterenol-induced phosphorylation of Thr17-PLN, normalized to total PLN, was fully inhibited by RA306 in a dose-dependent manner, with IC50s of 140 nM in rat, 205 nM in mouse, and 220 nM in human cardiomyocytes.

RA608 (RA-608) is a potent, selective, ATP-competitive, orally available CaMKII inhibitor, inhibits human CaMKIIδ, CaMKIIγ, CaMKIIα, and CaMKIIβ with IC50 of 22, 51, 121, and 1135 nM, respectively.RA608 displays a good selectivity profile against a broad panel of 304 human recombinant kinases.RA608 significantly reduces SR Ca leak in human atrial cardiomyocytes, reduces diastolic tension of human atrial trabeculae, does not affect action potential characteristics; attenuates heart failure in the murine HF model induced by TAC.

SD-36 (STAT3 degrader SD-36) is a potent, selective STAT3 degrader (PROTAC), potently induces the degradation of STAT3 protein in vitro and in vivo.SD-36 is designed using an analogue of CRBN ligand lenalidomide and the STAT3 inhibitor SI-109, binds to recombinant STAT3 protein with Ki of 11 nM.SD-36 (250 nM) depleted >90% of STAT3 protein in MOLM-16 cells after 4 hr treatment and >50% of STAT3 protein in DEL, KI-JK and SU-DHL-1 cells after 7 hr treatment, also efficiently degraded STAT3 protein in murine cells.SD-36 displays extremely high cellular selectivity for degradation of STAT3 over other STATs.SD-36 effectively degrades both wild-type and mutated STAT3 proteins in cells, effectively degrades mutated STAT3 (D661Y, K658R mutant), also effectively degrades CRISPR-mutated homozygous Y705F mutant STAT3 protein in DLD-1/STAT3Y705F/Y705F cells.SD-36 displayed strong growth-inhibitory activities in a subset of leukemia and lymphoma cell lines (MOLM-16 cell line IC50, 35 nM), 100-fold more potent than SI-109.SD-36 (i.v. 25 mg/kg) effectively and selectively depletes STAT3 protein, achieves complete and long-lasting tumor regression in in mouse xenograft tumors.

SHP2 PROTAC R1-5C is a potent and highly selective SHP2 PROTAC created by conjugating RMC-4550 with pomalidomide using a PEG linker, with a low nanomolar DC50; SHP2 PROTAC R1-5C is highly selective for SHP2, induces degradation of SHP2 in leukemic cells at submicromolar concentrations. SHP2 PROTAC R1-5C inhibits MAPK signaling, and suppresses cancer cell growth. SHP2 PROTACs serve as an alternative strategy for targeting ERK-dependent cancers and are useful tools alongside allosteric inhibitors for dissecting the mechanisms by which SHP2 exerts its oncogenic activity.

SMN2 splicing modulator TEC-1 is a novel specific, CNS penetrant small molecule SMN2 splicing modulator, increases the expression level of FL-SMN2 mRNA and decreases the expression level of Δ7 mRNA.TEC-1 showed higher selectively (>60-fold) on galactosylceramidase and huntingtin gene expression compared to previously reported compounds (e.g., SMN-C3) due to off-target effects on cryptic exon inclusion and nonsense-mediated mRNA decay.TEC-1 modulates SMN2 splicing and displays disease-modifying effects in motor neurons derived from SMA patient iPSCs (GM24468).|TEC-1 rescues the phenotype in a murine model of spinal muscular atrophy (SMA).

SP23 is a STING protein degrader (PROTAC) based on a small-molecule STING inhibitor (C-170) and pomalidomide (a CRBN ligand), shows degradation potency with DC50 of 3.2 uM.SP23 exerted high anti-inflammatory efficacy in a cisplatin-induced acute kidney injury mouse model by modulating the STING signaling pathway.

SY2-062 is a thalidomide derivative and useful precursor for synthesis of thalidomide-based PROTAC degrader.

Thailanstatin B is a potent antiproliferative natural product and pre-mRNA splicing inhibitor, potential antibody-drug conjugate payload.

Thailanstatin D (TST-D) is a potent antiproliferative natural product and direct precursor of Thailanstatin A, inhibits eukaryotic RNA splicing with stiong anti-tumor activities.Thailanstatin D inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and Thailanstatin D preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site.Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis.Thailanstatins are attractive cytotoxin agent for ADC design.

TIM-063 (TIM063) is a potent, selective, ATP-competitive CaMKK inhibitor with Ki of 0.35/0.2 uM for CaMKKα and CaMKKβ, respectively.TIM-063 directly targets the catalytic domain of CaMKK, similar to STO-609.TIM-063 suppressed the ionomycin-induced phosphorylation of exogenously expressed CaMKI, CaMKIV, and endogenous AMPKα in HeLa cells with an IC50 of 0.3 uM.TIM-063 suppressed CaMKK isoform-mediated CaMKIV phosphorylation in transfected COS-7 cells.TIM-063 displayed cell permeability and the ability to inhibit CaMKK activity in cells. TIM-063 is a useful chemical probe for the precise analysis of CaMKK-mediated signaling pathways.

UHMCP1 is a small molecule that prevents the SF3b155/U2AF65 interaction, binds to the hydrophobic pocket of the U2AF65 UHM domain (Kd=1-20 uM), impacts splicing and cell viability.

Wbox2 is a membrane-permeant peptide that potently inhibits clathrin-mediated endocytosis (CME, IC50=3 uM), binds to SNX9 and AP2 and perturbs clathrin interactions with AP2 and SNX9.Wbox2 has no effect on cell viability at ≤30 uM and exhibited an IC50 for cytotoxicity (>40 uM) that is 10-fold higher than that needed to inhibit CME.Wbox2 interferes with AP2–clathrin interactions and alters CCP dynamics, binds to both AP2 and SNX9 with binding affinities of 4.0 and 26.2 uM.

YOK-1304 AUTOTAC intermidate 1 is an intermidate for AUTOTAC design.

YOK-1304 is a small molecule p62-ZZ domain ligand, activate p62-dependent selective macroautophag, used for AUTOTAC design.AUTOphagy-TArgeting Chimera (AUTOTAC) is a general chemical tool and platform technology, which employs bifunctional molecules composed of target-binding ligands linked to autophagy-targeting ligands.AUTOTACs bind the ZZ domain of the otherwise dormant autophagy receptor p62/Sequestosome-1/SQSTM1, which is activated into oligomeric bodies in complex with targets for their sequestration and degradation.

YOK-2204 is a small molecule p62-ZZ domain ligand, activate p62-dependent selective macroautophag, used for AUTOTAC design.

YOK-2204 linker conjugate 1 is a PEG linker added to p62-ZZ ligand YOK-2204 for AUTOTAC design.

YTK-105 is a small molecule p62-ZZ domain ligand, activate p62-dependent selective macroautophag, used for AUTOTAC design.

YTK-105 linker conjugate 1 is a PEG linker added to p62-ZZ ligand YTK-105 for AUTOTAC design.

YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.

YX-2-115 is a palbociclib derivative compound with piperazine-linker tail for PROTAC YX-2-107 synthesis, inhibits CDK6 with IC50 of 4.5 nM.

YX-A-1 is a small-molecule modulator of human islet amyloid polypeptide (hIAPP) assembly, specifically enhances amyloid formation; YX-A-1 accelerates wt hIAPP assembly, even when added in substoichiometric concentration ratios (e.g. at a peptide:YX-A-1 molar ratio of 1:0.5 the t50 is reduced ~1.5-fold). YX-A-1 is a useful chemical tools to study hIAPP aggregation.

YX-I-1 is a small-molecule modulator of human islet amyloid polypeptide (hIAPP) assembly, specifically inhibits amyloid formation; YX-I-1 inhibits the aggregation of wt hIAPP, extending the t50 from 15.1 ± 0.2 h to 23.4 ± 1.0 h at a 1:7 molar ratio of peptide:inhibitor. YX-I-1 inhibits primary nucleation, secondary nucleation and elongation of wt hIAP. YX-A-1 is a useful chemical tools to study hIAPP aggregation.

ARN22089 (ARN 22089) is a specific small molecule inhibitor of putative CDC42 family effector interaction, binds to CDC42 and has broad anti-cancer activity and inhibits MAPK and S6 signaling.ARN22089 could inhibit CDC42-PAK interactions with EC50 of 0.1 uM, and inhibit RHOJ/PAK interactions with approximate EC50 of 1-5 uM.ARN22089 has a single-digit micromolar IC50 activity against sensitive cell lines (WM3248, SKMel3, A375, and SW480), has IC50 of < 10 uM for 55/100 cell lines in a panel of 100 cancer cell lines with various different mutations, including several cell lines with neuroblastoma RAS (NRAS) mutations.ARN22089 inhibits MAPK and S6 phosphorylation and influences NFkB signaling in vitro.ARN22089 specifically inhibits tumor angiogenesis in 3D vascularized microtumors, shows drug-like properties and inhibits tumor growth in vivo.ARN22089 selectively binds and inhibits CDC42 effector interactions.ARN22089 binds better to the purified CDC42 compared with other known CDC42 inhibitors (ZCL278, ML141, R-ketoralac, and Casin).CDC42 family GTPases (RHOJ, RHOQ, CDC42) are linked to multiple human cancers and modulate cell-cycle progression, tumor cell migration/invasion, and tumor angiogenesis.

H-Tyr(SO2F)-OMe-18F, a 18F-fluorosulfurylated phenol, is a positron emission tomography (PET) tracer.

Colibactin is a complex secondary metabolite produced by some genotoxic gut Escherichia coli strains. Colibactin has the potential for the research of colorectal cancer.

Tropatepine is an orally active, anticholinergic muscarinic antagonist and can be used as an antiparkinsonian agent. Tropatepine is used to combat against extrapyramidal syndrome induced by neuroleptic drugs.

(+)-3-Carene, a bicyclic monoterpene, is one of the major components of the pine tree essential oils. (+)-3-Carene is a (+)-enantiomer of 3-Carene.

Azapropazone is a nonsteroidal anti-inflammatory drug (NSAID). Azapropazone can be used for the research of rheumatoid arthritis and other rheumatoid conditions.

Azintamide (Bilipurum) can be used for the research of psoriasis vulgaris, dyspepsia and other conditions.

Cannabicitran is a cannabinoid. Cannabicitran can decrease intraocular pressure in rabbits.

Cyanidin-3-O-arabinoside is a pigment isolated from flowers of Rhododendron cv. Lems Stormcloud.

Fluridone is an inhibitor of abscisic acid (ABA) biosynthesis. Fluridone suppresses the expression of AchnFAR and TF genes and reduces the formation of primary alcohols.

LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases.

Neoamygdalin is a compound identified in the different processed bitter almonds. Neoamygdalin has the potential for the research of cough and asthma.

Pirifibrate (EL-466) is a hypolipemic substance. Pirifibrate can be used for the research of hyperlipoproteinemias.

Pyraflufen-ethyl is a phenylpyrazole herbicide for control of annual and perennial broadleaf weeds.

TH5427 is a promising, targeted inhibitor that can be used to further study NUDT5 activity and ADP-ribose metabolism. TH5427, blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells. NUDT5 is recently identified as a rheostat of hormone-dependent gene regulation and proliferation in breast cancer cells.

Thalidomide-piperazine hydrochloride has the potential for the research of leprosy and multiple myeloma. Thalidomide-piperazine hydrochloride used as a tool in developmental biology leads to important discoveries in the biochemical pathways of limb development.

(S,S)-BD-AcAc 2 ((S,S)-Ketone Ester) is a (S,S)-enantiomer of BD-AcAc 2. BD-AcAc 2 elevates the AcAc and acetone levels, thereby produces sustained ketosis and significantly delays central nervous system oxygen toxicity (CNS-OT) seizures.

11-trans Leukotriene E4 is an isomer of Leukotriene E4 (LTE4). Slow isomerization of the C-11 double bond of LTE4 leads to the formation of 11-trans LTE4. 11-trans Leukotriene E4 is equipotent to LTE4 in contracting guinea pig ileum.

13-Hydroxylupanine (Hydroxylupanine) is the typical alkaloid profile of sweet lupins.13-Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle.

14:0 DAP (1,2-dimyristoyl-3-dimethylammonium-propane ) is a cationic lipid that can be used for drug delivery.

16-Epiestriol is a metabolite of the endogenous estrogen estrone with antibacterial and anti-inflammatory effects.

4BAB (compound 29) is an irreversible glyoxalase I (GLO1) inhibitor. 4BAB has anticancer effects.

4-Hydroxyhippuric acid is a by-product of metabolism of polyphenols and increases the microflora activity related to the refeeding.

6-trans-leukotriene B4 is a neutrophil chemotaxin in the guinea pig dermis.

Alendronate sodium is an orally active nitrogen-containing bisphosphonate. Alendronate sodium potently inhibits bone resorption. Alendronate sodium is used for the research of postmenopausal osteoporosis.

Aucuparin, a natural product found in Sorbus aucuparia, inhibits pulmonary fibrosis in a bleomycin (BLM)-induced lung fibrosis mouse model. Anti-inflammatory activity.

BAY-R 1005, an immunoenhancing agent, is a synthetic glycolipid analogue (GLA), which is supposed to modulate antibody synthesis.

Bilirubin Conjugate disodium is a ditaurate derivative of Bilirubin. Bilirubin, a major end product of heme breakdown, is an important constituent of bile.

CCW16 is the covalent ligand for the E3 ubiquitin ligase RNF4. CCW16 can be used in the synthesis of protein degraders.

Coumarin hydrazine is a fluorescent chemical probe (λex=420–450/λem=468 nm) to label cellular protein- and lipid-bound carbonyls.

Croverin is a diterpenoid compound isolated from the aerial parts of Croton laui.

CS12192 is a compound improving survival and weight gain. CS12192 has the potential for the research of graft-versus-host disease (GVHD) (extracted from the patent CN112773802A).

Cussosaponin C is a compound isolated from Pulsatilla koreana Nakai.

Cyclobutyrol is a potent choleretic agent. Cyclobutyrol also inhibits biliary lipid secretion. Cyclobutyrol induces choleretic is unrelated to bile acids. CB and bile acids do not compete for the hepatobiliar transport mechanisms

DAUDA (11-(dansylamino) undecanoic acid) is an environment-sensitive fluorescent fatty acid analogue. DAUDA alters its intensities and fluorescent emission spectra on entry into binding proteins. DAUDA is used to determine the relative affinity of natural fatty acids for polymorphs of the Schistosoma mansoni Sm14 fatty acid-binding protein.

Deschloro Cetirizine Dihydrochloride is a Cetirizine impurity. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist.

EDMPC, a cationic lipid, has an enhanced ability to deliver DNA to pulmonary tissues. EDMPC mediates intralobar DNA delivery to rodents.

Emylcamate is a potent muscle relaxant. Emylcamate has the potential for the research of neurological diseases.

EUK-118 is an analog of EUK 8 and EUK 134 with reduced activity. EUK-118 exhibits superoxide dismutase (SOD) mimetic activity.

Fenadiazole acts as a central nervous system agent to manage insomnia and dreaminess.

Fenquizone (MG-13054), a thiazide-like diuretic, exhibits chronic antihypertensive effect. Fenquizone can be used for the research of oedema and hypertension.

Flocoumafen (WL 108366), a second-generation anticoagulant rodenticide (ARs), belongs to the family of vitamin K antagonist (VKA) molecules.

Fluorescent DOTAP, a cationic lipid, can be used for the research of nucleic acid and protein delivery.

Glycolithocholic acid sodium is the sodium salt of Glycolithocholic acid. Glycolithocholic acid is a glycine-conjugated secondary bile acid. Glycolithocholic acid can be used to diagnose ulcerative colitis (UC), non-alcoholic steatohepatitis (NASH) and primary sclerosing cholangitis (PSC).

GP3269 is a potent, selective, and orally active inhibitor of human adenosine kinase (AK) with an IC50 of 11 nM. GP3269 exhibits anticonvulsant activity in rats.

Green CMFDA (CMFDA) is a cell-permeable fluorescent probe that can be used a cell tracer. Green CMFDA can be cleaved by non-specific esterases common to living cells, producing a fluorescent compound, fluorescein, visible using a fluorescent microscope.

H-Glu(Met-OH)-OH could induce oxidation of hydroxyl radical.

Inositol nicotinate, with vasodilatory effect, is used in the study of Peripheral arterial disease (PAD).

Jineol is a cytotoxic alkaloid from the centipede Scolopendra subspinipes. Jineol exhibits modest cytotoxic activity in vitro against the growth of human tumor cell lines.

Levatin is an 18-Norclerodane diterpene from Croton levatii.

Linoleyl methane sulfonate is a selective lipid-based vehicle for use in drug delivery systems.

Loliolide, a Carotenoid Metabolite, is a potential endogenous inducer of herbivore resistance. Loliolide also inhibits the seedling growth.

Makisterone A, a 28-carbon moulting hormone, has been identified as the major free pupal ecdysteroid in the honey bee, Apis mellifera.

Maresin 2 is an anti-inflammatory and pro-resolving mediator from human macrophages. Maresins are a new family of anti-inflammatory and pro-resolving lipid mediators biosynthesized from docosahexaenoic acid (DHA) by macrophages.

MitoPerOx is a fluorescent ratio-probe of lipid peroxidation. MitoPerOx can be taken up very rapidly into mitochondria within cells, thereby responding to changes in mitochondrial lipid peroxidation.

MitoTracker Green FM is a green-fluorescent dye that can selectively accumulate in the mitochondrial matrix. MitoTracker Green FM covalently binds to mitochondrial proteins by reacting with free thiol groups of cysteine residues.

MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.

MRS4620 is a potent CD73 inhibitor, with a Ki of 0.436 nM. MRS4620 can be use for the research of cancer immunotherapy.

Nonacosadiene is the pheromone of Drosophila melanogaster from a tetrahydrophyridine derivative.

OB-24 is a potent inhibitor of heme oxygenase-1 (HO-1). Heme oxygenase-1, a member of the heat shock protein family, plays a key role as a sensor and regulator of oxidative stress. OB-24 significantly inhibited cell proliferation in vitro and tumor growth and lymph node/lung metastases in vivo. OB-24 has potential for the research of advanced prostate cancer (PCA).

Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs.

Pseudoisocyanine (iodide) is a pan inhibitor of monoamine transporters and organic cation transporters with antidepressant-like activity.

Resolvin E2 ((-)-Resolvin E2), a proresolving lipid mediator, is useful as a lead for anti-inflammatory agent.

Saponin PE is a saponin compound isolated from aerial part of Clematis tangutica.

Sorbicillin, a sorbicillinoid analogue, acts as a potent anti-inflammation agent.

SQDG is a glycolipid that possesses sugar moieties in their head groups. SQDG is a membrane lipid that can be used to investigate the effects of structural lipid in LNP formulations.

Suc-Gly-Pro-AMC is a fibroblast activation protein (FAP)-specific substrate. Suc-Gly-Pro-AMC can be used to study the activity of FAP.

Sulfo-GMBS is a cross-linker. Among the amine-sulfhydryl cross-linkers, Sulfo-GMBS generated the largest number of cross-links and covered most of the cross-links that were identified with AMAS and GMBS.

Transfectam is a cationic lipid able to interact with DNA to form complexes that mediate efficient gene transfer into various eukaryotic cells.

UDP-GalNAz disodium (UDP-N-azidoacetylgalactosamine disodium) is the analogue of UDP-GalNAc. UDP-GalNAc is the donor substrate of many N-acetylgalactosaminyltransferases, enzymes which transfer GalNAc from the nucleotide sugar to a saccharide or peptide acceptor.

Y29 is a potent PFKFB3 inhibitor with an IC50 of 0.183 µM, and acts as a competitive inhibitor against Fru-6-P with a Ki of 0.094 µM. Y29 also inhibits the HeLa cell growth with a GI50 of 2.7 µM.

β-L-Fucopyranosyl phosphate can be used for the research of carbohydrate metabolism. Glycosyl phosphates play crucial roles in carbohydrate metabolism as metabolic regulators or ubiquitous intermediates for glycoconjugate biosynthesis.

CATPB is a potent, selective free fatty acid receptor 2 (FFA2R/GPR43) antagonist.

Metapramine (19560 RP) is an antidepressant agent, belonging to the class of tricyclic compounds. Metapramine inhibits norepinephrine reuptake, without affecting the reuptake of serotonin or dopamine. Metapramine is a low-affinity antagonist of the N-methyl-D-aspartic acid (NMDA) receptor complex channel.

Etoxadrol (CL-1848C) is a potent N-methyl-D-aspartic acid (NMDA) antagonist with high affinity. Etoxadrol can be used for anaesthetic research.

Dioxone is a substance possessing convulsant properties qualitatively similar to leptazol and bemegride. Dioxone is orally active.

VY-3-135 is an orally active, selective acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC50 value of 44 nM. VY-3-135 displayes no inhibitory activity towards recombinant human ACSS1 or ACSS3. VY-3-135 potently inhibits ACSS2 dependent fatty acid metabolism but has no effect on gene expression in tumors. VY-3-135 inhibits triple negative breast cancer (TNBC) tumor growth in mouse ACSS2high but not ACSS2low tumors models.

IP2 is an immunomodulatory agent. IP2 increases PTP (Pioneer Translation Product)-derived antigen presentation in cancer cells. IP2 shows non-cytotoxic for cancer cells. IP2 induces tumor growth defects in mouse.

GSK329 is a potent and selective diarylurea inhibitor of the cardiac-specific kinase TNNI3K. GSK329 exhibits positive cardioprotective outcomes in the model of ischemia/reperfusion cardiac injury.

Y-29794 (Compound 2) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a Ki of 0.95 nM. Y-29794 can be used for studying neurodegenerative diseases and cancer.

HTS07545 is a potent sulfide:quinone oxidoreductase (SQOR) inhibitor with an IC50 of 30 nM. HTS07545 decrease the rate of breakdown of hydrogen sulfide (H2S). HTS07545 can be used for heart failure research.

SH-42 is a potent and selective inhibitor of human Δ24-dehydrocholesterol reductase (DHCR24), with an IC50 of 42 nM. SH-42 can lead to a significant increase in plasma desmosterol levels of mice.

Hit 1 is an activator of ansulin degrading enzyme (IDE), with an EC50 of 5.5 μM. Hit 1 can decrease glucose-stimulating insulin secretion.

Dexelvucitabine (Reverset), a cytidine analog, is a nucleoside reverse transcriptase inhibitor. Dexelvucitabine is a powerful drug against HIV-1-resistant viruses containing a thymidine analog and/or M184V mutation in the viral polymerase. Dexelvucitabine is a 2′-deoxycytidine antiretroviral agent.

Boc-L-Ala-OH-15N is the 15N labeled Boc-L-Ala-OH.

Droxidopa-13C2,15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood–brain barrier.

KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization.

Deac-SS-Biotin is a potent antitumor agent. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity.

GSD-11 is a potent and selective anti-austerity agent. GSD-11 inhibits the cell migration and colony formation of PANC-1 cells. GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 has the potential for the research of pancreatic cancer.

Fluocortin butyl ester is a developed corticosteroid compound with no detectable systemic corticosteroid activity when it is used topically. Fluocortin butyl ester appears to be an effective well-tolerated topical steroid useful in the research of perennial rhinitis.

Letosteine is an orally active, potent and safe expectorant. Letosteine dissolves bronchial mucus and reduces respiratory inflammation symptoms, and restores gas exchanges and natural defense mechanisms in the lung. Letosteine can be used for acute or chronic respiratory diseases (such as bronchopneumopathies) research.

Antiproliferative against-4 (comp 4) shows the highest potency for MCF-7 cells (IC50 = 0.19 nM).

Yakuchinone A, a natural product isolated from Alpinia oxyphylla Miquel (Zingiberaceae), has strong inhibitory effects on the synthesis of prostaglandins (PGs) and leukotrienes (LTs).

HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells.

Garcinielliptone HD is a compound isolated from the heartwood of Garcinia subelliptica Merr. .

2-Chloro-N6-furfuryladenine is a Kinetin riboside derivative.

(E)-Isoconiferin is a compound synthesized from vanillin, syringaldehyde, and p-hydroxybenzaldehyde, by five reaction steps in high overall yield.

TCS 2210 (compound 1) is a neuronal differentiation inducer in mesenchymal stem cells (MSCs). TCS 2210 increases expression of the neuronal markers β-III tubulin and neuron-specific enolase (NSE).

DL-2-Amino-3-(hydroxy-amino)propionic acid-15N is a 15N-labeled DL-2-Amino-3-(hydroxy-amino)propionic acid.

PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.

Fmoc-L-Val-OH-15N is a 15N-labeled Leucomalachite green. Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen[1][2].

NIOCH 14 is a antiviral agent and a pro-drug. NIOCH 14 has antiviral activity against orthopoxviruses. NIOCH 14 can significantly lower proportions of infected mice, and virus production levels in the lungs. NIOCH 14 can be used for researching anti-smallpox.

Cyclic HPMPC is a potent antiviral agent. Cyclic HPMPC can increase arterial oxygen saturation levels in lethal vaccinia virus (IHD strain)-infected mice. Cyclic HPMPC improves the outcome of congenital guinea pig cytomegalovirus (GPCMV) infection and decreases viral replication in guinea pig model.

γ-L-Glutamyl-S-allyl-L-cysteine is a naturally occurring organosulfur compound found in garlic.

YSK 05 is a pH-sensitive cationic lipid. YSK 05 improves the intracellular trafficking of non-viral vectors. YSK 05-MEND shows significantly good gene silencing activity and hemolytic activity. YSK 05 overcomes the suppression of endosomal escape by PEGylation. YSK 05 effectively enhances siRNA delivery both in vitro and in vivo.

BPC157 (Bepecin, PL 14736), a small, chemically synthesised pentadecapeptide and a partial sequence of the human gastric juice protein BPC, which has been shown to be safe in clinical trials for inflammatory bowel disease and may be able to cure intestinal anastomosis dehiscence.

Dammarenediol II (Compound 3) is a compound isolated from the resin of Boswellia freerana.

Cannabisin B (Compound 7) is a compound isolated from the aerial part of Tetragonia tetragonioides (New Zealand spinach).

Xanthine-15N2 is a 15N-labeled Lauroyl-L-carnitine (chloride).

(R)-1-PeCSO (trans-(+)-S-1-Propenyl-L-cysteine sulfoxide) is the most abundant flavor precursor in onions.

6bK is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK increases circulating insulin in high-fat-fed mice. Acute administration of 6bK enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice.

MT-VC-ZD02044 is a cytotoxic and anti-mitotic agent.

TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion.

Fmoc-Glu(OtBu)-OH-15N is a 15N-labeled Fmoc-L-Val-OH.

Fissitungfine B is a compound extracted from the tropical medicinal plant Fissistigma tungfangense. Fissitungfine B has strong anticancer activity.

Fmoc-Pro-OH-15N is a 15N-labeled Glycine ethyl ester monohydrochloride.

NHS-NH-(diethylamino)ethyl benzoate is a compound that can be used for N-glycan labeling.

1-Octylnonyl 8-[[8-[(1-ethylnonyl)oxy]-8-oxooctyl](2-hydroxyethyl)amino]octanoate is a PEG lipid. 1-Octylnonyl 8-[[8-[(1-ethylnonyl)oxy]-8-oxooctyl](2-hydroxyethyl)amino]octanoate can be used for researching drug delivery.

Photosensitizer-2 (compound 1) is a organic D-π-A sensitizer against phototoxicity. Photosensitizer-2 contains an acrylic acid moiety that exerts high levels of phototoxicity. Photosensitizer-2 shows antitumor activity against HeLa cells, with IC50 values of 20.9 ± 4.5 μM (dark) and 0.046 ± 0.012 μM (irradiation), respectively.

ThioD is a protein linker with a hydrophobic thioester.

SGC-AAK1-1N is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor, with an IC50 of 1.8 μM.

LRH-1 modulator-1 (compound 6N) is a potent LRH-1 (liver receptor homolog-1) modulator/agonist. LRH-1 modulator-1 shows anti-inflammatory effects in intestinal organoids. LRH-1 modulator-1 induces anti-inflammatory cytokine IL-10, and reduces inflammatory cytokine IL-1b and TNFa.

Grosshemin (Grosshemine) is a natural compound found in the Siberian population of Centaurea scabiosa.

Acridone-4-carboxylic acid (ACA) (Compound 2c) is a heme-interacting acridone derivatives that prevents free heme-mediated protein oxidation and degradation. Acridone-4-carboxylic acid inhibits protein carbonyl formation with an IC50 of 43 μM.

BB 0305179 (compound 59) is a potent anti-prion agent, with an IC50 of 4.7 μM. BB 0305179 inhibits the toxicity of a specific PrP mutant carrying a deletion in the hydrophobic domain .

O-Acetylgalanthamine, a acetylated alkaloid, is a natural product that can be isolated from Narcissus pseudonarcissus.

FAP-2286, a fibroblast activation protein (FAP)-binding peptidic macrocycle coupled to the radionuclide chelator DOTA. FAP-2286 has potent affinity to human FAP protein with a Kd of 1.1 nM. FAP-2286, a tumor imaging agent, is a useful tool for the research of positron emission tomography (PET). FAP-2286 has antitumor activity.

PAL-4 (compound 4) is a potent, selective and reversible Lysophospholipase-like 1 (LYPLAL1) activator with EC50 value of 0.39 μM and 0.49 μM for mice LYPLAL1 and huamn LYPLAL1, respectively. PAL-4 can be used for researching metabolic disorders.

Cepharanoline is a compound isolated from Stephania cepharantha Hayata. Cepharanoline has proliferative activities.

Nicomol is an orally active hypolipidemic agent that can increase the high density lipoprotein cholesterol (HDL-C) level. Nicomol inhibits the rapid rise of plasma free fatty acids.

Lucenin-2 is a natural C-glucoside compound belonging to the flavonoid class.

Quercetin 3-O-rutinoside-7-O-glucoside (compound 8) is an antioxidant agent that canbe found in Hemerocallis fulva. Quercetin 3-O-rutinoside-7-O-glucoside shows strong lipid peroxidation inhibitory activities.

PEAQX ((1RS,1'S)-PEAQX, NVP-AAM077) is an effective and orally available human NMDA antagonist, which shows preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over hNMDA 1A/2B receptors (IC50=29,600 nM).

N-Methylflindersine is a compound isolated as insect antifeedants from the East African Rutaceous medicinal plants Fagara chalybea and F. holtziana.

Piperitol is a compound isolated from the Tibetan medicinal plant Lancea tibetica.

Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM, can be used for the research of metastatic prostate cancer.

Cararosinol A is a compound isolated from the roots of Caragana sinica.

Primulic acid I (Primulasaponin 1) is a plant-derived triterpenoid saponin with one sugar chain (monodesmoid).

Ornoprostil is a prostaglandin E1 analogue. Ornoprostil is orally active and can be used for gastric ulcer research.

Verrucosin (Compound 3) is a compound isolated from Myristica fragrans.

Obovatol is a biphenyl ether lignan isolated from the leaves of Magnolia obovata Thunb.

Dieckol, is a naturally occurring phlorotannin found in some brown algal species. Dieckol has anti-bacterial, anti-cancer, anti-oxidant, anti-aging, anti-diabetic, neuroprotective actions.

INI-43, a Kpnβ1 inhibitor, interferes with the nuclear localization of Kpnβ1 and known Kpnβ1 cargoes, NFAT, NFκB, AP-1 and NFY.

Iopentol is a non-ionic, intravascular contrast media.

Campneoside II is a compound isolated from Paulownia tomentosa var. tomentosa wood. Campneoside II exhibits excellent anti-complement activity.

SQM-NBD is a potent and selectiveAIE fluorescent probe. SQM-NBD exhibits excellent sensitivity to Cys and Hcy with the LOD of 54 nM and 72 nM, respectively.SQM-NBD has good cell permeability and low cytotoxicity. SQM-NBD has the potential for Cys/Hcy identification under physiological and pathological conditions.

SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity.

Epitizide, a benzothiadiazine, commonly found in combination Triamterene, is used to produce diuresis.

2-Nitrophenanthraquinone is a bioactive compound.

Exo2 is a secretion inhibitor. Exo2 perturbs trafficking of Shiga toxin between endosomes and the trans-Golgi network. Exo2 blocks secretory cargo exit from the ER (endoplasmic reticulum) and disrupts the Golgi apparatus, but does not affect the morphology of the TGN (trans-Golgi network) Exo2 can stimulate calcium-dependent exocytosis in permeabilized adrenal chromaff in cells.

Fluorescein octadecyl ester is a lipophilic fluorescent reagent is immobilized in a plasticized PVC membrane. Fluorescein octadecyl ester can reversibly recognize alcohol molecules and can be used to determine the concentration of ethanol in alcoholic drinks. Fluorescein octadecyl ester can be used as acceptor to make optrode membrane for the determination of picric acid.

BODIPY-8-chloromethane is a fluorophore. BODIPY-8-chloromethane can be used as as a fluorescent probe.

Insulin lispro is a recombinant human insulin analogue and is one of three rapid-acting insulin analogues available. Insulin lispro can be used for the research of hyperglycaemia in diabetes mellitus.

NHS-SS-Ac is an amine-reactive product synthesized from acetic acid.

5,5'-Difluoro BAPTA is the most widely used probe for studying cytosolic free Ca2+ by 19F NMR. 5,5'-Difluoro BAPTA has high selectivity for Ca2+. 5,5'-Difluoro BAPTA can inhibit the growth of pollen tube.

β-S-ARCA is a mRNA 7-methylguanosine (m7G) cap analog carrying a phosphorothioate (PS) moiety. mRNAs incorporating β-S-ARCA have elongated cellular half-lives and showed augmented protein expression. β-S-ARCA D1 has been applied in researching experimental mRNA-based anticancer vaccines.

Haloperidol lactate is a potent antipsychotic agent. Haloperidol lactate can be used in acute and chronic schizophrenia and gilles de la tourette's syndrome. Haloperidol lactate has the potential for the research of psychotic disorders.

SG3400 delate (Mal-amido-PEG8) (compound 21) is an intermediate for the synthesis of ADC molecules. SG3400 delete is an effective toxin molecule with anticancer activity. SG3400 delete can be used in cancer research.

N-Acryloyl-1-pyrenebutylamine is a potent fluorescent derivatization agent. N-Acryloyl-1-pyrenebutylamine combines with an alkyl-acrylamide side-chain to give fluorescence function on the polymer..

Cavutilide, benzamide, is used as an antiarrhythmic, antiarythmique.

N-Butylfluorescein is an alkyl-substituted fluorescein, can be used for synthesis of fluorogenic substrates for assaying phosphatidylinositol-specific phospholipase C.

Lafadofensine D-(-)-Mandelic acid is the monoamines reuptake inhibitor. Lafadofensine D-(-)-Mandelic acid has sufficient effects after short-term administration.

Fosimdesonide, a small molecule of adalimumab fosimdesonide, is a potent immunomodulator. Fosimdesonide shows anti-inflammatory activity.

Opadotina is a small molecule of anvatabart opadotin. Opadotina shows antineoplastic activity.

Tazide is an antineoplastic agent.

(R)-GNE-274 is a enantiomer of GNE-274. GNE-274 is a non-degrader that is structurally related to GDC-0927 (estrogen receptor degrader).

Nifuraldezone-15N3 is the 15N3 labeled Nifuraldezone.

SRI-37330 hydrochloride is an orally bioavailable thioredoxin-interacting protein (TXNIP) inhibitor. SRI-37330 hydrochloride inhibits glucagon secretion and function, reduces hepatic glucose production and reverses hepatic steatosis. SRI-37330 hydrochloride can be used for type 2 diabetes research.

Brogidirsen exerts the stimulatory function of synthesis of functional dystrophin.

(Rac)-CFT7455 is a zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3) degrader, acting via the ubiquitin proteasome pathway, with a GI50 of 0.05 nM for NCIH929.1 cells. (Rac)-CFT7455 is the racemic isomer of CFT7455 which is a IKZF1/IKZF3 degrader with anticancer activity.

1-Heptadecanoyl-2-eicosatrienoyl-sn-glycero-3-phospho- L-serine-d5 (sodium) is deuterium labeled 1-Heptadecanoyl-2-eicosatrienoyl-sn-glycero-3-phospho- L-serine (sodium).