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(67)
- DNA Damage/DNA Repair(45)
- PI3K/Akt/mTOR Signaling(35)
- Microbiology & Virology(42)
- Cell Cycle/Checkpoint(150)
- Ubiquitination/ Proteasome(21)
- JAK/STAT Signaling(9)
- TGF-β / Smad Signaling(11)
- GPCR/G protein(3)
- Stem Cell(17)
- Membrane Transporter/Ion Channel(161)
- Cancer Biology(321)
- Endocrinology and Hormones(119)
- Obesity, Appetite Control & Diabetes(9)
- Peptide Inhibitors and Substrate(1)
- Other Signal Transduction(81)
- Vitamin D Related(0)
- Antibody-drug Conjugate/ADC Related(0)
- Ox Stress Reagents(22)
Products for Signaling Pathways
- Cat.No. Product Name Information
- GC19566 N-Nitrosodiethylamine
NLRP3 inflammasome inhibitor
- GC63267 α-Chaconine
α,β-Methyleneadenosine 5'-triphosphate (sodium salt)
α,β-Methyleneadenosine 5'-triphosphate (αβ-methylene ATP) is a phosphonic analog of ATP that is characterized by the replacement of the bridging oxygen atom between the α- and β-phosphate groups with methylene.
Bacteria synthesize the cellular growth factor putrescine through a number of pathways.
- GC63268 α-Amyrin palmitate
α-Carotene is a precursor of vitamin A that has been found in various fruits and vegetables.
- GC63269 α-Conotoxin PIA TFA
- GC63723 α-Conotoxin PnIA TFA
- GC39464 α-Cyclodextrin
α-D-Galactopyranosylphenyl isothiocyanate is a chemically activated form of galactose that has been used to prepare various neoglycoproteins, which consist of a glycosylated serum albumin substituted with either fluorescein or methotrexate.
α-Ecdysone is a prohormone of 20-hydroxy ecdysone, an insect-molting, ecdysteroid hormone.
- GC38042 α-Factor Mating Pheromone, yeast (TFA)
α-GalCer analog 8
α-Galactosylceramide analog 8 (α-GalCer analog 8) is a triazole derivative of α-galactosylceramide.
- GC45207 α-hydroxy Farnesyl Phosphonic Acid α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase).
- GC45208 α-hydroxy Metoprolol α-hydroxy Metoprolol is an active metabolite of the β1-adrenergic receptor blocker metoprolol.
- GC45210 α-Linolenic Acid (sodium salt) α-Linolenic acid (ALA) is an essential fatty acid found in leafy green vegetables.
- GC45601 α-Linolenic Acid ethyl ester-d5
- GC45602 α-Linolenic Acid-d5 MaxSpec• Standard
- GC63749 α-Lipoic Acid-d5
α-Muricholic acid is a murine-specific primary bile acid.
- GC45213 α-NETA Choline acetyltransferase (ChAT) mediates the synthesis of the neurotransmitter acetylcholine from acetyl-CoA and choline.
- GC41499 α-Phellandrene α-Phellandrene is a cyclic monoterpene that has been found in various plants, including Cannabis, and has diverse biological activities.
- GC40480 α-Phenyl-α-(2-pyridyl)acetonitrile α-Phenyl-α-(2-pyridyl)thioacetamide, also known as antigastrin and SC-15396, is an inhibitor of gastric acid secretion.
- GC38287 α-Pyridone
- GC63941 α-Solanine
- GC41501 α-Terpinene α-Terpinene is a terpenoid that has been found in Cannabis and has diverse biological activities, including acaricidal, antiprotozoal, and antioxidant properties.
- GC63615 α-Thujone
- GC37980 α-Tocopherol phosphate
α-Truxillic acid can be formed by the dimerization of two molecules of α-trans-cinnamic acid.
- GC40753 α-Zearalanol α-Zearalanol is an active metabolite formed by reduction of α-zearalenol, an estrogen receptor antagonist.
- GC38873 α2β1 Integrin Ligand Peptide TFA
- GC62380 αvβ1 integrin-IN-1
- GC62566 αvβ1 integrin-IN-1 TFA
- GC49467 β-Aescin A triterpenoid saponin with diverse biological activities
- GC63273 β-Amyloid (1-14),mouse,rat
- GC63274 β-Amyloid (1-42), (rat/mouse) (TFA)
- GC37984 β-Amyloid (1-42), rat
- GC61394 β-Amyloid (1-42), rat TFA
- GC37991 β-Amyloid 15-21
- GC45603 β-Amyrin
- GC45225 β-Apooxytetracycline β-Apooxytetracycline is a potential impurity found in commercial preparations of oxytetracycline.
- GC60391 β-Casomorphin, bovine TFA
- GC61484 β-Casomorphin, human TFA
- GC62432 β-catenin-IN-2
- GC40789 β-Cembrenediol β-Cembrenediol (β-CBT) is a natural product from tobacco plants that is found in cigarette smoke condensate.
- GC63275 β-Cryptoxanthin
Hydrogen sulfide (H2S) is a naturally-occurring gasotransmitter with vasodilator and inflammatory modulating activity.
- GC63276 β-Cyclocitral
- GC45228 β-Cyclodextrin β-Cyclodextrin (β-CD) is a cyclic oligosaccharide that contains seven D-(+)-glucopyranose units and has been used to improve the aqueous solubility of various compounds, especially those containing a phenyl group.
- GC63277 β-Cyclogeraniol
- GC45232 β-D-Glucosamine Pentaacetate β-D-Glucosamine pentaacetate is an N-acetylglucosamine derivative that has been shown to promote hyaluronic acid production.
D-Glucose, a naturally occurring monosaccharide found in plants, is the primary energy source for living organisms.
- GC63278 β-D-Glucose pentaacetate
- GC45230 β-Defensin-3 (human) (trifluoroacetate salt) β-Defensin-3 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.
- GC45231 β-Defensin-4 (human) (trifluoroacetate salt) β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.
- GC41623 β-Elemonic Acid β-Elemonic acid is a triterpene isolated from Boswellia (Burseraceae) that exhibits anticancer activity.
- GC45234 β-Endorphin (1-27) (human) (trifluoroacetate salt) β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors).
- GA24007 β-Endorphin (30-31) (bovine, camel, mouse, ovine) The dipeptide Gly-Gln, which is naturally derived from the posttranslational processing of β-endorphin, exhibited an inhibitory action on cell firing when applied iontophoretically to brainstem neurons in the rat. Moreover, it seems to be a neurotrophic regulator of acetylcholinesterase in the mammalian sympathetic ganglion. Gly-Gln suppressed morphine withdrawal symptoms in rats. Gly-Gln has found use as a Gln source in parenteral nutrition, see also G-1210.
- GC45236 β-Endorphin (rat) β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities.
- GC38030 β-Endorphin, equine (TFA)
- GC62551 β-Hydroxypropiovanillone
- GC49647 β-Hyodeoxycholic Acid (hydrate) A 3β epimer of hyodeoxycholic acid
- GC62235 β-Lactamase-IN-2
- GC38007 β-Melanocyte Stimulating Hormone (MSH), human TFA
- GC40719 β-Muricholic Acid A murine-specific primary bile acid
- GC41502 β-Myrcene β-Myrcene is a terpene that has been found in Cannabis and has antioxidative properties.
- GC45604 β-Rubromycin
- GC38008 β-Zearalenol
- GC61462 γ-1-Melanocyte Stimulating Hormone (MSH), amide
- GC38010 γ-Aminobutyric acid
- GC40551 γ-CEHC The major tocopherol obtained from natural dietary sources is γ-tocopherol, whereas α-tocopherol is the form of Vitamin E typically obtained from synthetic supplements.
- GC63279 γ-Glu-Gly TFA
- GC63280 γ-Hexalactone
- GC40790 γ-Linolenic Acid ethyl ester γ-Linolenic acid (GLA) is an ω-6 fatty acid which can be elongated to arachidonic acid for endogenous eicosanoid synthesis.
- GC41503 γ-Terpinene γ-Terpinene is a monoterpene that has been found in various plants, including C.
- GC41109 δ12-Prostaglandin J2 δ12-PGJ2 is a decomposition product of PGD2 in aqueous media in the presence of albumin.
- GC45238 δ14-Triamcinolone acetonide δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide.
- GC45239 δ4-Abiraterone δ4-Abiraterone (D4A) is an active metabolite of the CYP17A1 inhibitor abiraterone.
- GC62708 σ1 Receptor antagonist-1
- GC41552 ω-3 Arachidonic Acid ω-3 Arachidonic acid is a rare PUFA found in trace amounts in dietary sources.
- GC41393 ω-3 Arachidonic Acid methyl ester ω-3 Fatty acids, represented primarily by docosahexaenoic acid, eicosapentaenoic acid, and α-linoleate, are essential dietary nutrients required for normal growth and development.
- GC62067 ω-Conotoxin GVIA TFA
- GA24016 ω-Conotoxin MVIIA ω-Conotoxin MVIIA, originally isolated from the venom of the fish-hunting cone snail Conus magus, is a blocker of voltage-sensitive Ca²? channels in neurons. The peptide has been used to identify different Ca²? channel subtypes in amphibian brain.
- GC63281 ω-Pentadecalactone
- GC62478 Ζ-Stat-2
- GC45713 (±)-α-Tocopherol Acetate
- GC38194 (±)-10-Hydroxycamptothecin
- GC41657 (±)-2-Amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (hydrobromide) (±)-2-Amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (6,7-ADTN) is a dopamine receptor agonist (EC50s = 3.5 and 0.65 μM in rat striatal and nucleus accumbens homogenates, respectively).
- GC41658 (±)-2-hydroxy Ibuprofen (±)-2-hydroxy Ibuprofen is a metabolite of ibuprofen .
- GC41661 (±)-4-hydroxy Propranolol β-D-Glucuronide (±)-4-hydroxy Propranolol β-D-glucuronide is a metabolite of (±)-4-hydroxy propranolol, which is a metabolite of propranolol.
- GC40559 (±)-Alliin Alliin is a cysteine sulfoxide constituent of garlic that is converted by alliinase to allicin, which imparts its pungent aroma and flavor.
- GC62726 (±)-Amiflamine
- GC34961 (±)-BI-D
- GC41668 (±)-Clopidogrel (hydrochloride) Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM).
- GC60394 (±)-Duloxetine hydrochloride
- GC41669 (±)-Enterolactone Diets high in fiber contain plant lignan species that may be directly responsible for some observed health benefits of these diets.
- GC41670 (±)-Epinephrine (hydrochloride) (±)-Epinephrine is a natural neurotransmitter that is released from the adrenal medulla and activates adrenoceptors (Kis = 15, 735, and 3,970 nM for α1A-, β2-, and β1-adrenergic receptors, respectively).
(±)-Equol 4'-sulfate (sodium salt)
(±)-Equol 4'-sulfate is a gut-mediated phase II metabolite of the isoflavonoid phytoestrogen (±)-equol.