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Signaling Pathways

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.

References:

[1] Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.

[2] Peters C, et al. Biosci Rep. 2015 Jun 12;35(4). pii: e00225. doi: 10.1042/BSR20150089.

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  1. Cat.No. Product Name Information
  2. GC19789 Hyaluronidase

     Hyaluronidase;>300u/mg

     Hyaluronidase  Chemical Structure
  3. GC63267 α-​Chaconine α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level.  α-​Chaconine  Chemical Structure
  4. 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. α-?Terpinyl acetate  Chemical Structure
  5. GC65446 α-Amyrin acetate α-Amyrin acetate, a natural triterpenoid, has anti-inflammatory activity, antispasmodic profile and the relaxant effect. α-Amyrin acetate  Chemical Structure
  6. GC63268 α-Amyrin palmitate α-Amyrin palmitate is isolated from Santalum album (sandalwood). α-Amyrin palmitate  Chemical Structure
  7. GC49097 α-Conotoxin AuIB (trifluoroacetate salt) A conotoxin and an antagonist of α3β4 subunit-containing nAChRs α-Conotoxin AuIB (trifluoroacetate salt)  Chemical Structure
  8. 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. α-Conotoxin GI  Chemical Structure
  9. GC49140 α-Conotoxin ImI (trifluoroacetate salt) A conotoxin and an antagonist of α7 nAChRs α-Conotoxin ImI (trifluoroacetate salt)  Chemical Structure
  10. GC63269 α-Conotoxin PIA TFA α-Conotoxin PIA TFA  Chemical Structure
  11. GC52338 α-Conotoxin PnIA (trifluoroacetate salt) A peptide antagonist of α3β2-subunit containing and α7 nAChRs α-Conotoxin PnIA (trifluoroacetate salt)  Chemical Structure
  12. GC63723 α-Conotoxin PnIA TFA α-Conotoxin PnIA TFA  Chemical Structure
  13. GC49838 α-Cortolone A metabolite of cortisol α-Cortolone  Chemical Structure
  14. GC52253 α-Enolase (1-19)-biotin Peptide A biotinylated α-enolase peptide α-Enolase (1-19)-biotin Peptide  Chemical Structure
  15. GC70181 α-Glucosidase-IN-22

    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.

    α-Glucosidase-IN-22  Chemical Structure
  16. 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. α-Helical CRF(9-41) TFA  Chemical Structure
  17. GC67685 α-Isopropylmalate α-Isopropylmalate  Chemical Structure
  18. 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. α-Ketoglutaric Acid (sodium salt)  Chemical Structure
  19. GC63749 α-Lipoic Acid-d5 α-Lipoic Acid-d5  Chemical Structure
  20. 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. α-Lipoic acid-NHS  Chemical Structure
  21. 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. α-Methyl-p-tyrosine  Chemical Structure
  22. GC64563 α-Methylserotonin α-Methylserotonin  Chemical Structure
  23. GC49008 α-Muricholic Acid-d4 An internal standard for the quantification of α-muricholic acid α-Muricholic Acid-d4  Chemical Structure
  24. 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. α-Solanine  Chemical Structure
  25. GC63615 α-Thujone α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone  Chemical Structure
  26. 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. α-Tocopherol phosphate disodium  Chemical Structure
  27. GC68390 α5β1 integrin agonist-1 α5β1 integrin agonist-1  Chemical Structure
  28. GC70179 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.

    α7 Nicotinic receptor agonist-1  Chemical Structure
  29. 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. αvβ1 integrin-IN-1  Chemical Structure
  30. GC62566 αvβ1 integrin-IN-1 TFA αvβ1 integrin-IN-1 TFA  Chemical Structure
  31. GC64932 αvβ5 integrin-IN-1 αvβ5 integrin-IN-1 is a first potent and selective αvβ5 integrin inhibitor (pIC50 = 8.2) . αvβ5 integrin-IN-1  Chemical Structure
  32. GC49467 β-Aescin A triterpenoid saponin with diverse biological activities β-Aescin  Chemical Structure
  33. GC63273 β-Amyloid (1-14),mouse,rat β-Amyloid (1-14),mouse,rat  Chemical Structure
  34. 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) (TFA)  Chemical Structure
  35. GC70182 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).

    β-Amyloid (1-40), FAM-labeled TFA  Chemical Structure
  36. GC63274 β-Amyloid (1-42), (rat/mouse) (TFA) β-Amyloid (1-42), (rat/mouse) (TFA)  Chemical Structure
  37. 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). β-Amyloid (22-35) (TFA)  Chemical Structure
  38. 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. β-Amyloid (42-1), human TFA  Chemical Structure
  39. 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. β-Amyrone  Chemical Structure
  40. GC48920 β-Carboline-1-carboxylic Acid An alkaloid with diverse biological activities β-Carboline-1-carboxylic Acid  Chemical Structure
  41. GC61484 β-Casomorphin, human TFA β-Casomorphin, human TFA  Chemical Structure
  42. 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. β-catenin-IN-2  Chemical Structure
  43. GC63275 β-Cryptoxanthin β-Cryptoxanthin ((3R)-β-Cryptoxanthin), isolated from Satsuma mandarin orange, is an oxygenated carotenoid and a potent antioxidant. β-Cryptoxanthin  Chemical Structure
  44. GC63276 β-Cyclocitral β-Cyclocitral, a volatile oxidized derivative of β-carotene, is a grazer defence signal unique to the Cyanobacterium Microcystis. β-Cyclocitral  Chemical Structure
  45. GC63277 β-Cyclogeraniol β-Cyclogeraniol is a natural odour compound. β-Cyclogeraniol  Chemical Structure
  46. 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. β-D-Glucan  Chemical Structure
  47. GC63278 β-D-Glucose pentaacetate β-D-Glucose Pentaacetate (Penta-O-acetyl-β-D-glucopyranose) is used in biochemical reaction. β-D-Glucose pentaacetate  Chemical Structure
  48. 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). β-D-glucuronide-pNP-carbonate  Chemical Structure
  49. GC48998 β-Defensin-1 (human) (trifluoroacetate salt) An antimicrobial peptide β-Defensin-1 (human) (trifluoroacetate salt)  Chemical Structure
  50. GC52494 β-Endorphin (rat) (trifluoroacetate salt) An opioid neuropeptide β-Endorphin (rat) (trifluoroacetate salt)  Chemical Structure
  51. 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. β-Estradiol-6-one 6-(O-carboxymethyloxime)  Chemical Structure
  52. GC49769 β-Glucogallin A plant metabolite and an aldose reductase 2 inhibitor β-Glucogallin  Chemical Structure
  53. GC64430 β-Glucuronidase-IN-1 β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. β-Glucuronidase-IN-1  Chemical Structure
  54. GC49890 β-Glycerophosphate-d5 (sodium salt hydrate) An internal standard for the quantification of β-glycerophosphate β-Glycerophosphate-d5 (sodium salt hydrate)  Chemical Structure
  55. 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. β-Hydroxypropiovanillone  Chemical Structure
  56. GC49647 β-Hyodeoxycholic Acid (hydrate) A 3β epimer of hyodeoxycholic acid β-Hyodeoxycholic Acid (hydrate)  Chemical Structure
  57. GC64619 β-Ionone β-Ionone is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity. β-Ionone  Chemical Structure
  58. GC62235 β-Lactamase-IN-2 β-Lactamase-IN-2 is a beta-lactamase inhibitor, extracted from patent WO 2019075084 A1, compound 1. β-Lactamase-IN-2  Chemical Structure
  59. 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). β-Methylcrotonyl coenzyme A lithium  Chemical Structure
  60. GC49007 β-Muricholic Acid-d4 An internal standard for the quantification of β-muricholic acid β-Muricholic Acid-d4  Chemical Structure
  61. GC70184 β-Naphthoflavone-CH2-Br

    Beta-naphthoflavone-CH2-Br is an aryl hydrocarbon receptor (AhR) ligand. It is used in the synthesis of PROTAC Beta-NF-JQ1.

    β-Naphthoflavone-CH2-Br  Chemical Structure
  62. 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. β-Nicotinamide adenine dinucleotide reduced dipotassium  Chemical Structure
  63. GC70185 β-Sitostenone

    Beta-sitostenone is a sterol isolated from Cochlospermum vitifolium. It can inhibit the activity of tyrosinase and has anti-melanogenesis and anti-tumor activities.

    β-Sitostenone  Chemical Structure
  64. GC61462 γ-1-Melanocyte Stimulating Hormone (MSH), amide γ-1-Melanocyte Stimulating Hormone (MSH), amide  Chemical Structure
  65. GC64508 γ-Aminobutyric acid-d6

    γ-Aminobutyric acid-d6 (4-Aminobutyric acid-d6) is the deuterium labeled γ-Aminobutyric acid.

    γ-Aminobutyric acid-d6  Chemical Structure
  66. GC49865 γ-D-Glutamylglycine (trifluoroacetate salt) An excitatory amino acid antagonist γ-D-Glutamylglycine (trifluoroacetate salt)  Chemical Structure
  67. GC52400 γ-Glu-Ala (trifluoroacetate salt) A dipeptide γ-Glu-Ala (trifluoroacetate salt)  Chemical Structure
  68. GC63279 γ-Glu-Gly TFA γ-Glu-Gly TFA  Chemical Structure
  69. GC52404 γ-Glu-Phe (trifluoroacetate salt) A dipeptide with metabolism-altering activity γ-Glu-Phe (trifluoroacetate salt)  Chemical Structure
  70. GC70186 γ-Glutamylornithine

    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.

    γ-Glutamylornithine  Chemical Structure
  71. GC63280 γ-Hexalactone γ-Hexalactone is a gamma-lactone found in ripe fruits. γ-Hexalactone  Chemical Structure
  72. 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. δ-Secretase inhibitor 11  Chemical Structure
  73. GC62708 σ1 Receptor antagonist-1 σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1  Chemical Structure
  74. GC70188 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.

    ω-Agatoxin IVA TFA  Chemical Structure
  75. GC62067 ω-Conotoxin GVIA TFA ω-Conotoxin GVIA TFA  Chemical Structure
  76. GC64899 ω-Conotoxin MVIIC TFA ω-Conotoxin MVIIC TFA  Chemical Structure
  77. GC49009 ω-Muricholic Acid-d4 An internal standard for the quantification of ω-MCA ω-Muricholic Acid-d4  Chemical Structure
  78. GC63281 ω-Pentadecalactone ω-Pentadecalactone is a fragrance ingredient. ω-Pentadecalactone  Chemical Structure
  79. GC49296 τ-Fluvalinate A pyrethroid acaricide τ-Fluvalinate  Chemical Structure
  80. 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. (±)-α-Tocopherol nicotinate  Chemical Structure
  81. GC52010 (±)-10-hydroxy-12(Z),15(Z)-Octadecadienoic Acid An oxylipin gut microbiota metabolite (±)-10-hydroxy-12(Z),15(Z)-Octadecadienoic Acid  Chemical Structure
  82. GC52013 (±)-10-hydroxy-12(Z)-Octadecenoic Acid An oxylipin and metabolite of linoleic acid (±)-10-hydroxy-12(Z)-Octadecenoic Acid  Chemical Structure
  83. GC52421 (±)-10-hydroxy-12(Z)-Octadecenoic Acid-d5 An internal standard for the quantification of (±)-10-hydroxy-12(Z)-octadecenoic acid (±)-10-hydroxy-12(Z)-Octadecenoic Acid-d5  Chemical Structure
  84. GC62726 (±)-Amiflamine (±)-Amiflamine (FLA 336) is a potent monoamine oxidase-A (MAO-A) inhibitor with a pIC50 of 5.57. (±)-Amiflamine  Chemical Structure
  85. GC52260 (±)-Cenobamate An Analytical Reference Standard (±)-Cenobamate  Chemical Structure
  86. GC48923 (±)-Hydroxycitric Acid A hydroxy derivative of citric acid (±)-Hydroxycitric Acid  Chemical Structure
  87. GC49515 (±)-Ibuprofen-d3 (sodium salt) An internal standard for the quantification of (±)-ibuprofen (±)-Ibuprofen-d3 (sodium salt)  Chemical Structure
  88. GC65599 (±)-Leucine-d10 (±)-Leucine-d10  Chemical Structure
  89. GC52224 (±)-MMT5-14 A derivative of remdesivir with antiviral activity (±)-MMT5-14  Chemical Structure
  90. GC49875 (±)-N-desmethyl Venlafaxine (hydrochloride) A minor active metabolite of venlafaxine (±)-N-desmethyl Venlafaxine (hydrochloride)  Chemical Structure
  91. GC49482 (±)-Nornicotine-d4 An internal standard for the quantification of (±)-nornicotine (±)-Nornicotine-d4  Chemical Structure
  92. GC62727 (±)-Penbutolol-d9 hydrochloride (±)-Penbutolol-d9 ((Rac)-Penbutolol-d9) hydrochloride is a deuterium labeled (±)-Penbutolol hydrochloride. (±)-Penbutolol-d9 hydrochloride  Chemical Structure
  93. GC67928 (±)-Stylopine hydrochloride (±)-Stylopine hydrochloride  Chemical Structure
  94. GC64007 (±)-U-50488 hydrate hydrochloride (±)-U-50488 hydrate hydrochloride  Chemical Structure
  95. GC67681 (αR,8aS)-GSK1614343 (αR,8aS)-GSK1614343  Chemical Structure
  96. GN10155 (+)- Corydaline (+)- Corydaline  Chemical Structure
  97. GN10612 (+)- Praeruptorin C (+)- Praeruptorin C  Chemical Structure
  98. GC49268 (+)-δ-Cadinene A sesquiterpene with antimicrobial and anticancer activities (+)-δ-Cadinene  Chemical Structure
  99. GN10745 (+)-Bicuculline

    (+)-Bicucline is a competitive GABAA receptor antagonist with an IC50 of 2μM.

    (+)-Bicuculline  Chemical Structure
  100. GC64752 (+)-Biotin-ONP (+)-Biotin-ONP is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. (+)-Biotin-ONP  Chemical Structure
  101. GC66864 (+)-Biotin-PEG2-hydrazide (+)-Biotin-PEG2-hydrazide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. (+)-Biotin-PEG2-hydrazide  Chemical Structure

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