The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. The three components of the ADC together give rise to a powerful oncolytic agent capable of delivering normally intolerable cytotoxins directly to cancer cells, which then internalize and release the cell-destroying drugs. At present, two ADCs, Adcetris and Kadcyla, have received regulatory approval with >40 others in clinical development.
ADCs are administered intravenously in order to prevent the mAb from being destroyed by gastric acids and proteolytic enzymes. The mAb component of the ADC enables it to circulate in the bloodstream until it finds and binds to tumor-specific cell surface antigens present on target cancer cells. Linker chemistry is an important determinant of the safety, specificity, potency and activity of ADCs. Linkers are designed to be stable in the blood stream (to conform to the increased circulation time of mAbs) and labile at the cancer site to allow rapid release of the cytotoxic drug. First generation ADCs made use of early cytotoxins such as the anthracycline, doxorubicin or the anti-metabolite/antifolate agent, methotrexate. Current cytotoxins have far greater potency and can be divided into three main groups: auristatins, maytansines and calicheamicins.
The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especially promising path to improving ADC design, which will open the way for novel cancer therapeutics.
 Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.
 Peters C, et al. Biosci Rep. 2015 Jun 12;35(4). pii: e00225. doi: 10.1042/BSR20150089.
Targets for Signaling Pathways
- MAPK Signaling(26)
- Tyrosine Kinase(73)
- DNA Damage/DNA Repair(49)
- PI3K/Akt/mTOR Signaling(38)
- Microbiology & Virology(42)
- Cell Cycle/Checkpoint(168)
- Ubiquitination/ Proteasome(24)
- JAK/STAT Signaling(10)
- TGF-β / Smad Signaling(21)
- GPCR/G protein(3)
- Stem Cell(19)
- Membrane Transporter/Ion Channel(161)
- Cancer Biology(366)
- Endocrinology and Hormones(152)
- Obesity, Appetite Control & Diabetes(17)
- Peptide Inhibitors and Substrate(2)
- Other Signal Transduction(156)
- Vitamin D Related(0)
- Antibody-drug Conjugate/ADC Related(0)
- Ox Stress Reagents(24)
Products for Signaling Pathways
- Cat.No. Product Name Information
- GC63267 α-Chaconine α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level.
- GC66197 α-?Terpinyl acetate α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM.
- GC65446 α-Amyrin acetate α-Amyrin acetate, a natural triterpenoid, has anti-inflammatory activity, antispasmodic profile and the relaxant effect.
- GC63268 α-Amyrin palmitate α-Amyrin palmitate is isolated from Santalum album (sandalwood).
- GC49097 α-Conotoxin AuIB (trifluoroacetate salt) A conotoxin and an antagonist of α3β4 subunit-containing nAChRs
- GC26093 α-Conotoxin GI α-Conotoxin GI, a 13-residue peptide originally isolated from the venom of the fish-hunting cone snail Conus geographus, acts as a competitive antagonist for the muscle-type nicotinic acetylcholine receptor (nAChR) with excellent selectivity for α/δ receptor subunit binding over α/γ.
- GC49140 α-Conotoxin ImI (trifluoroacetate salt) A conotoxin and an antagonist of α7 nAChRs
- GC63269 α-Conotoxin PIA TFA
- GC52338 α-Conotoxin PnIA (trifluoroacetate salt) A peptide antagonist of α3β2-subunit containing and α7 nAChRs
- GC63723 α-Conotoxin PnIA TFA
- GC49838 α-Cortolone A metabolite of cortisol
- GC52253 α-Enolase (1-19)-biotin Peptide A biotinylated α-enolase peptide
Alpha-glucosidase-IN-22 (compound 7i) is a benzimidazole, an effective inhibitor of alpha-glucosidase with an IC50 of 0.64 μM. Alpha-glucosidase-IN-22 is an effective anti-diabetic active molecule with potential for use in type 2 diabetes (T2DM) research.
- GC66088 α-Helical CRF(9-41) TFA α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC50 of 140 nM.
- GC67685 α-Isopropylmalate
- GC48948 α-Ketoglutaric Acid (sodium salt) α-Ketoglutaric Acid (sodium salt) (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle.
- GC63749 α-Lipoic Acid-d5
- GC67540 α-Lipoic acid-NHS α-Lipoic acid-NHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
- GC65892 α-Methyl-p-tyrosine α-Methyl-p-tyrosine is a competitive inhibitor of the enzyme tyrosine hydroxylase, which converts tyrosine to Levodopa (DOPA). α-Methyl-p-tyrosine is an orally active inhibitor of catecholamine synthesis which inhibits the hydroxylation of tyrosine to DOPA.
- GC64563 α-Methylserotonin
- GC49008 α-Muricholic Acid-d4 An internal standard for the quantification of α-muricholic acid
- GC63941 α-Solanine α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in potatoes, has been observed to inhibit growth and induce apoptosis in cancer cells.
- GC63615 α-Thujone α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities.
- GC67618 α-Tocopherol phosphate disodium α-Tocopherol phosphate (alpha-Tocopherol phosphate) disodium, a promising antioxidant, can protect against long-wave UVA1 induced cell death and scavenge UVA1 induced ROS in a skin cell model. α-Tocopherol phosphate disodium possesses therapeutic potential in the inhibition of apoptosis and increases the migratory capacity of endothelial progenitor cells under high-glucose/hypoxic conditions and promotes angiogenesis.
- GC68390 α5β1 integrin agonist-1
α7 Nicotinic receptor agonist-1
Alpha-7 Nicotinic receptor agonist-1 (Preparation 5) is an alpha-7 nAChR agonist. It can be used for research on psychiatric disorders such as schizophrenia, mania or bipolar disorder, and anxiety disorders, as well as intellectual disabilities such as Alzheimer's disease, learning deficits, cognitive impairments, attention deficits, memory loss, Lewy body dementia and attention deficit hyperactivity disorder.
- GC62380 αvβ1 integrin-IN-1 αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM.
- GC62566 αvβ1 integrin-IN-1 TFA
- GC64932 αvβ5 integrin-IN-1 αvβ5 integrin-IN-1 is a first potent and selective αvβ5 integrin inhibitor (pIC50 = 8.2) .
- GC49467 β-Aescin A triterpenoid saponin with diverse biological activities
- GC63273 β-Amyloid (1-14),mouse,rat
- GC66089 β-Amyloid (1-40) (TFA) β-Amyloid (1-40) TFA is a primary protein in plaques found in the brains of patients with Alzheimer's disease.
β-Amyloid (1-40), FAM-labeled TFA
Beta-amyloid (1-40), FAM-labeled TFA is a FAM fluorescently labeled beta-amyloid (1-40) peptide (Λex= 492 nm and Λem= 518 nm).
- GC63274 β-Amyloid (1-42), (rat/mouse) (TFA)
- GC66416 β-Amyloid (22-35) (TFA) β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
- GC66346 β-Amyloid (42-1), human TFA β-Amyloid (42-1), human TFA is the inactive form of Amyloid β Peptide (1-42). β-Amyloid (42-1), human TFA is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
- GC66340 β-Amyrone β-Amyrone (β-Amyron) is a triterpene compound which has anti-inflammatory activity through inhibiting the expression of COX-2. β-Amyrone has antifungal activity , as well as antiviral activity against Chikungunya virus. β-Amyrone also inhibits α-glucosidase and acetylcholinesterase (AChE) activity. β-Amyrone can be used in the research of disease like inflammation, infection, and obesity.
- GC48920 β-Carboline-1-carboxylic Acid An alkaloid with diverse biological activities
- GC61484 β-Casomorphin, human TFA
- GC62432 β-catenin-IN-2 β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer.
- GC63275 β-Cryptoxanthin β-Cryptoxanthin ((3R)-β-Cryptoxanthin), isolated from Satsuma mandarin orange, is an oxygenated carotenoid and a potent antioxidant.
- GC63276 β-Cyclocitral β-Cyclocitral, a volatile oxidized derivative of β-carotene, is a grazer defence signal unique to the Cyanobacterium Microcystis.
- GC63277 β-Cyclogeraniol β-Cyclogeraniol is a natural odour compound.
- GC66870 β-D-Glucan β-D-glucan is a natural non-digestible polysaccharide and high biocompatibility that can be selectively recognized by recognition receptors such as Dectin-1 and Toll-like receptors as well as being easily internalized by murine or human macrophages, which is likely to attribute to a target delivery. β-d-glucan is an enteric delivery vehicle for probiotics.
- GC63278 β-D-Glucose pentaacetate β-D-Glucose Pentaacetate (Penta-O-acetyl-β-D-glucopyranose) is used in biochemical reaction.
- GC66750 β-D-glucuronide-pNP-carbonate β-D-glucuronide-pNP-carbonate is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
- GC48998 β-Defensin-1 (human) (trifluoroacetate salt) An antimicrobial peptide
- GC52494 β-Endorphin (rat) (trifluoroacetate salt) An opioid neuropeptide
- GC66512 β-Estradiol-6-one 6-(O-carboxymethyloxime) β-Estradiol-6-one 6-(O-carboxymethyloxime) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
- GC49769 β-Glucogallin A plant metabolite and an aldose reductase 2 inhibitor
- GC64430 β-Glucuronidase-IN-1 β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E.
- GC49890 β-Glycerophosphate-d5 (sodium salt hydrate) An internal standard for the quantification of β-glycerophosphate
- GC62551 β-Hydroxypropiovanillone β-Hydroxypropiovanillone, a natural compound, shows significant concentration-dependent inhibitory effects on α-glucosidase with an IC50 of 257.8 μg/mL.
- GC49647 β-Hyodeoxycholic Acid (hydrate) A 3β epimer of hyodeoxycholic acid
- GC64619 β-Ionone β-Ionone is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity.
- GC62235 β-Lactamase-IN-2 β-Lactamase-IN-2 is a beta-lactamase inhibitor, extracted from patent WO 2019075084 A1, compound 1.
- GC66842 β-Methylcrotonyl coenzyme A lithium β-Methylcrotonyl coenzyme A lithium is an intermediate in leucine metabolism and can be used as a substrate to study the specificity and kinetics of β-methylcrotonyl coenzyme A carboxylase (MCCase).
- GC49007 β-Muricholic Acid-d4 An internal standard for the quantification of β-muricholic acid
Beta-naphthoflavone-CH2-Br is an aryl hydrocarbon receptor (AhR) ligand. It is used in the synthesis of PROTAC Beta-NF-JQ1.
- GC67484 β-Nicotinamide adenine dinucleotide reduced dipotassium β-Nicotinamide adenine dinucleotide reduced dipotassium is an orally active reduced coenzyme. β-Nicotinamide adenine dinucleotide reduced dipotassium is a donor of ADP-ribose units in ADP-ribosylaton reactions and a precursor of cyclic ADP-ribose. β-Nicotinamide adenine dinucleotide reduced dipotassium plays a role as a regenerative electron donor in cellular energy metabolism, including glycolysis, β-oxidation and the tricarboxylic acid (TCA) cycle.
Beta-sitostenone is a sterol isolated from Cochlospermum vitifolium. It can inhibit the activity of tyrosinase and has anti-melanogenesis and anti-tumor activities.
- GC61462 γ-1-Melanocyte Stimulating Hormone (MSH), amide
- GC64508 γ-Aminobutyric acid-d6
- GC49865 γ-D-Glutamylglycine (trifluoroacetate salt) An excitatory amino acid antagonist
- GC52400 γ-Glu-Ala (trifluoroacetate salt) A dipeptide
- GC63279 γ-Glu-Gly TFA
- GC52404 γ-Glu-Phe (trifluoroacetate salt) A dipeptide with metabolism-altering activity
Gamma-glutamylornithine is a urine excretion product of patients with HHH syndrome (hyperuricemia, hyperammonemia, and homocitrullinuria) and patients with uric acid-related recurrent ataxia. Increased endogenous ornithine levels lead to an increase in gamma-glutamylornithine levels in the urine.
- GC63280 γ-Hexalactone γ-Hexalactone is a gamma-lactone found in ripe fruits.
- GC66048 δ-Secretase inhibitor 11 δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research.
- GC48532 ε-Rhodomycinone A bacterial metabolite and precursor to rhodomycin D
- GC62708 σ1 Receptor antagonist-1 σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28).
ω-Agatoxin IVA TFA
ω-Agatoxin IVA TFA is an effective selective blocker of P/Q-type Ca2+ (Cav2.1) channels, with IC50 values of 2 nM and 90 nM for P-type and Q-type Ca2+ channels, respectively. ω-Agatoxin IVA TFA (IC50, 30-225 nM) inhibits high potassium-induced glutamate release and calcium influx. It also blocks the release of serotonin and adrenaline induced by high potassium, without affecting L-type or N-type calcium channels.
- GC62067 ω-Conotoxin GVIA TFA
- GC64899 ω-Conotoxin MVIIC TFA
- GC49009 ω-Muricholic Acid-d4 An internal standard for the quantification of ω-MCA
- GC63281 ω-Pentadecalactone ω-Pentadecalactone is a fragrance ingredient.
- GC49296 τ-Fluvalinate A pyrethroid acaricide
- GC67191 (±)-α-Tocopherol nicotinate (±)-α-Tocopherol nicotinate, vitamin E - nicotinate, is an orally active fat-soluble antioxidant that prevents lipid peroxidation in cell membranes. (±)-α-Tocopherol nicotinate is hydrolysed in the blood to α -tocopherol and niacin and may be used in studies of related vascular diseases.
- GC52010 (±)-10-hydroxy-12(Z),15(Z)-Octadecadienoic Acid An oxylipin gut microbiota metabolite
- GC52013 (±)-10-hydroxy-12(Z)-Octadecenoic Acid An oxylipin and metabolite of linoleic acid
- GC52421 (±)-10-hydroxy-12(Z)-Octadecenoic Acid-d5 An internal standard for the quantification of (±)-10-hydroxy-12(Z)-octadecenoic acid
- GC62726 (±)-Amiflamine (±)-Amiflamine (FLA 336) is a potent monoamine oxidase-A (MAO-A) inhibitor with a pIC50 of 5.57.
- GC52260 (±)-Cenobamate An Analytical Reference Standard
- GC48923 (±)-Hydroxycitric Acid A hydroxy derivative of citric acid
- GC49515 (±)-Ibuprofen-d3 (sodium salt) An internal standard for the quantification of (±)-ibuprofen
- GC65599 (±)-Leucine-d10
- GC52224 (±)-MMT5-14 A derivative of remdesivir with antiviral activity
- GC49875 (±)-N-desmethyl Venlafaxine (hydrochloride) A minor active metabolite of venlafaxine
- GC49482 (±)-Nornicotine-d4 An internal standard for the quantification of (±)-nornicotine
- GC62727 (±)-Penbutolol-d9 hydrochloride (±)-Penbutolol-d9 ((Rac)-Penbutolol-d9) hydrochloride is a deuterium labeled (±)-Penbutolol hydrochloride.
- GC67928 (±)-Stylopine hydrochloride
- GC64007 (±)-U-50488 hydrate hydrochloride
- GC67681 (αR,8aS)-GSK1614343
- GN10155 (+)- Corydaline
- GN10612 (+)- Praeruptorin C
- GC49268 (+)-δ-Cadinene A sesquiterpene with antimicrobial and anticancer activities
(+)-Bicuculline is a light-sensitive competitive antagonist of GABA-A receptor.
- GC64752 (+)-Biotin-ONP (+)-Biotin-ONP is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.