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.
Targets for Signaling Pathways
- Proteases(63)
- Apoptosis(1189)
- Chromatin/Epigenetics(17)
- Metabolism(420)
- MAPK Signaling(32)
- Tyrosine Kinase(104)
- DNA Damage/DNA Repair(62)
- PI3K/Akt/mTOR Signaling(56)
- Microbiology & Virology(68)
- Cell Cycle/Checkpoint(205)
- Ubiquitination/ Proteasome(43)
- JAK/STAT Signaling(13)
- TGF-β / Smad Signaling(30)
- Angiogenesis(85)
- GPCR/G protein(3)
- Stem Cell(27)
- Membrane Transporter/Ion Channel(216)
- Cancer Biology(449)
- Endocrinology and Hormones(167)
- Neuroscience(463)
- Obesity, Appetite Control & Diabetes(8)
- Peptide Inhibitors and Substrate(1)
- Other Signal Transduction(140)
- Immunology/Inflammation(1111)
- Cardiovascular(63)
- Vitamin D Related(0)
- Antibody-drug Conjugate/ADC Related(0)
- PROTAC(218)
- Ox Stress Reagents(25)
- Others(4319)
- Antiparasitics(10)
- Toxins(88)
Products for Signaling Pathways
- Cat.No. Product Name Information
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GC72133
µ-Conotoxin-CnIIIC acetate
µ-Conotoxin-CnIIIC acetate, a 22-residue conopeptide, is a potent antagonist of the voltage-gated NaV1.4 sodium channel with an IC50 of 1.3 nM acting at the neuromuscular junction.
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GC71814
α-1-3,4 Fucosyltransferase, helicobacter pylori
α-1-3,4 Fucosyltransferase (α1,3/4FucT) (EC 2.4.1.65) (Hp3/4FT) can be found in Helicobacter pylori.
-
GC71815
α-2,3-Sialyltransferase, pasteurella multocida
alpha-2,3-Sialyltransferase (PmST3) (EC 2.4.99.4) is a beta-galactoside.
-
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.
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GC74347
α-Casozepine
α-Casozepine is a bioactive peptide derived from the α protein S1 casein in milk and has an affinity for γ-aminobutyric acid (GABA) receptors in the brain.
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GC72093
α-CGRP (mouse, rat) (TFA)
α-CGRP (mouse, rat) TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator.
-
GC72110
α-CGRP(human) TFA
α-CGRP(human) TFA is a regulatory neuropeptide of 37 amino acids.
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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.
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GC52338
α-Conotoxin PnIA (trifluoroacetate salt)
α-CtxPnIA, αPnIA
A peptide antagonist of α3β2-subunit containing and α7 nAChRs -
GC52253
α-Enolase (1-19)-biotin Peptide
Enolase-1 (1-19)-biotin
A biotinylated α-enolase peptide -
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.
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GC72710
α-Glucosidase-IN-35
α-Glucosidase-IN-35 (compound 1) is a kind of chromene.
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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.
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GC72837
α-Hydroxyglutaric acid-d4 disodium
2-Hydroxyglutarate-d4 disodium; 2-Hydroxyglutaric acid-d4 disodium; 2-Hydroxypentanedioic acid-d4 disodium
α-droxyglutaric acid-d4 (disodium) is the deuterium labeled α-droxyglutaric acid disodium. -
GC67685
α-Isopropylmalate
α-IPM
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GC67540
α-Lipoic acid-NHS
DL-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.
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GC67618
α-Tocopherol phosphate disodium
alpha-Tocopherol phosphate disodium; TocP disodium; Vitamin E 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
-
GC70953
α7 nAchR-JAK2-STAT3 agonist 1
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO).
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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.
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GC72246
αC-Conotoxin PrXA
αC-Conotoxin PrXA is a paralytic peptide neurotoxin and a competitive nAChR antagonist, with IC50s of 1.8 nM (α1β1εδ, adult) and 3.0 nM (α1β1γδ, fetal), respectively.
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GC71810
β-1,4-Galactosyltransferase, neisseria meningitides
beta-1,4-Galactosyltransferase (LgtB) (EC 2.4.1.90) (B4GALT1 (LgtB)) is often used in biochemical studies.
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GC70787
β-Aminoarteether
β-Aminoarteether (SM934 free base) is an Artemisinin derivative with orally active.
-
GC66089
β-Amyloid (1-40) (TFA)
Amyloid Beta-Peptide (1-40) (human) TFA; Amyloid β-Peptide (1-40) (human) TFA
β-Amyloid (1-40) TFA is a primary protein in plaques found in the brains of patients with Alzheimer's disease. -
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).
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GC66416
β-Amyloid (22-35) (TFA)
Amyloid β-Protein (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
Amyloid β Peptide (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. -
GC71998
β-Amyrin acetate
β-Amyrin acetate is a triterpenoid with potent anti-inflammatory, antifungal, anti-diabetic, anti-hyperlipidemic activities.
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GC66340
β-Amyrone
β-Amyron
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. -
GC71980
β-Caryophyllene-d2
β-Caryophyllene-d2 is deuterium labeled β-Caryophyllene.
-
GC72805
β-catenin-IN-6
β-catenin-IN-6 is a β-catenin inhibitor, targeting to canonical Wingless-related integration site signaling pathway.
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GC74300
β-CGRP (mouse)
Calcitonin gene-related peptide 2 (mouse); CGRP II (mouse
β-CGRP (mouse) is a calcitonin gene-related peptide that induces vasodilation. -
GC90496
β-Cortolone
A metabolite of cortisol
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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.
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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).
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GC72141
β-defesin 1 (pig) (TFA)
β-defesin 1 (pig) (pBD-1) TFA is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites.
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GC52494
β-Endorphin (rat) (trifluoroacetate salt)
An opioid neuropeptide
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GC72132
β-Endorphin, equine TFA
β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors.
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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.
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GC91530
β-Ionone Acid
β-Ionone acid is the acid form of the β-carotenoid derivative β-ionone.
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GC72123
β-Melanocyte Stimulating Hormone (MSH), human TFA
β-Melanocyte Stimulating Hormone (MSH), human TFA, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
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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).
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GC70184
β-Naphthoflavone-CH2-Br
β-NF-CH2-Br
Beta-naphthoflavone-CH2-Br is an aryl hydrocarbon receptor (AhR) ligand. It is used in the synthesis of PROTAC Beta-NF-JQ1.
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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.
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GC72061
β-Phellandrene
β-Phellandrene is obtained from Carum petroselinum.
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GC70185
β-Sitostenone
δ4-Sitosterol-3-one; β-Rosasterol oxide
Beta-sitostenone is a sterol isolated from Cochlospermum vitifolium. It can inhibit the activity of tyrosinase and has anti-melanogenesis and anti-tumor activities.
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GC70650
γ-Acetylenic GABA hydrochloride
γ-Acetylenic GABA (GAG) hydrochloride is an irreversible inhibitor of GABA-transaminase.
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GC52400
γ-Glu-Ala (trifluoroacetate salt)
γ-Glutamylalanine, γ-L-Glutamyl-L-alanine
A dipeptide -
GC52404
γ-Glu-Phe (trifluoroacetate salt)
γ-Glutamylphenylalanine
A dipeptide with metabolism-altering activity -
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.
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GC70796
γ-Glutamylserine
γ-Glutamylserine (γ-Glu-Ser) is a calcium receptor activator.
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GC92102
γ1-MSH (human, mouse, rat, bovine) (acetate)
γ1-Melanocyte-stimulating Hormone
γ1-Melanocyte-stimulating hormone (γ1-MSH) is a peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland. -
GC92101
γ1-MSH (human, mouse, rat, bovine) (trifluoroacetate salt)
γ1-Melanocyte-stimulating Hormone
γ1-Melanocyte-stimulating hormone (γ1-MSH) is a peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland. -
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.
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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.
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GC70556
ß-pBrPh-Glc
β-pBrPh-Glc is a small-molecule ice recrystallization inhibitor.
-
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.
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GC52421
(±)-10-hydroxy-12(Z)-Octadecenoic Acid-d5
10-hydroxy-cis-12-Octadecenoic Acid-d5
An internal standard for the quantification of (±)-10-hydroxy-12(Z)-octadecenoic acid -
GC52260
(±)-Cenobamate
An Analytical Reference Standard
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GC72801
(±)-Clopidogrel bisulfate
Clopidogrel sulfate is an antiplatelet agent.
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GC72625
(±)-Coniine hydrochloride
(±)-Coniine hydrochloride (2-Propylpiperidine hydrochloride) is a potent nAChR agonist with an EC50 value of 0.3 mM.
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GC91298
(±)-Linalool-d3
An internal standard for the quantification of (±)-linalool
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GC52224
(±)-MMT5-14
A derivative of remdesivir with antiviral activity
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GC90022
(±)-Norepinephrine-d6 (hydrochloride)
An internal standard for the quantification of norepinephrine
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GC90428
(±)-Pregabalin-13C3
An Analytical Reference Standard
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GC67928
(±)-Stylopine hydrochloride
Tetrahydrocoptisine hydrochloride
-
GC91065
(±)13,14-EDT
A metabolite of adrenic acid
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GC91067
(±)16,17-EDT
A metabolite of adrenic acid
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GC91574
(±)2-HOTrE
FA 18:3;O,(±)2-9(Z),12(Z),15(Z)-HOTrE,α-Hydroxylinolenic Acid,2-Hydroxylinolenic Acid,(±)-2-hydroxy-9(Z),12(Z),15(Z)-OTrE
(±)2-HOTrE is an oxylipin. -
GC73670
(αR)-Cyclopropaneacetamide-Exatecan
(αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, is a cytotoxic agent.
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GC67681
(αR,8aS)-GSK1614343
-
GN10155
(+)- Corydaline
(+)-Corydaline, D-Corydaline, NSC 406036
-
GN10612
(+)- Praeruptorin C
-
GN10745
(+)-Bicuculline
NSC 32192
(+)-Bicucline ((+)-Bicucline )) is a competitive GABAA receptor antagonist with an IC50 of 2μM. -
GC66864
(+)-Biotin-PEG2-hydrazide
(+)-Biotin-PEG2-hydrazide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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GC66692
(+)-Biotin-SLC
(+)-Biotin-SLC is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
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GN10605
(+)-Catechin hydrate
D-(+)-Catechin, Catechuic Acid, Cyanidol
-
GN10654
(+)-Corynoline
(+)-Corynoline, 13-methyl-Chelidonine, CRL, (d)-Corynoline
-
GC70265
(+)-EMD 57033
(+)-EMD 57033 is a cardiac troponin C (cTnC) activator, is a dominant Ca2+ sensitizer.
-
GC70332
(+)-Erinacin A
(+)-Erinacin A is an anticancer compound that can be isolated from the mushroom Hericium erinaceum.
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GC74247
(+)-Glaucarubinone
(+)-Glaucarubinone is a potent AP-1 (activator protein-1) inhibitor with an EC50 value of 0.13 µM.
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GC67931
(+)-Medioresinol
-
GC16616
(+)-MK 801
Dizocilpine maleate;Dizocilpine hydrogen maleate;(+)-MK 801;MK 801
-
GC91031
(+)-Muscarine (tosylate)
An Analytical Reference Standard
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GC68210
(+)-Norfenfluramine
-
GC74191
(+)-trans-Permethrin
(+)-trans-NRDC-143; (1R)-trans-Permethrin
(+)-trans-Permethrin ((+)-trans-NRDC-143) is a pyrethroid which is synthetic derivative of the natural toxins pyrethrins contained in the flowers of Chrysanthemum species. -
GC69720
(+)SHIN2
(+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, and its in vivo target can be traced using 13C-serine. (+)SHIN2 increases the survival rate of mice with primary acute T-cell lymphoblastic leukemia (T-ALL) driven by Notch1 and has a synergistic effect with Methotrexate.
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GC73658
(-)-5-HT2C agonist-3
(-)-5-HT2C agonist-3 (compound (–)-19) is a 5-HT2C selective agonist with Gq signaling preference, with EC50 values ??for 5-HT2 receptors of 5-HT2C: 103 nM; 5-HT2B: 570 nM; 5-HT2A: 72 nM.
-
GC71675
(-)-cis-Permethrin
(-)-cis-Permethrin is a pyrethroid insecticide widely used to control many common pests.
-
GC14049
(-)-Epigallocatechin gallate (EGCG)
EGCG
(-)-Epigallocatechin Gallate sulfate (EGCG) is a major polyphenol in green tea that inhibits cell proliferation and induces apoptosis. -
GC69463
(-)-GSK598809 hydrochloride
(1S,5R)-GSK598809 hydrochloride
(-)-GSK598809 is an isomer of GSK598809. GSK598809 is a selective antagonist of the dopamine D3 receptor (DRD3).
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GC71452
(-)-Hydroxycitric acid
(-)-Hydroxycitric acid (Garcinia acid) is the principal acid of fruit rinds of Garcinia cambogia.
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GC74197
(-)-Isoproterenol hydrochloride
Levisoprenaline hydrochloride; Proternol L hydrochloride
(-)-Isoproterenol (Levisoprenaline; Proternol L) drochloride is a β-adrenoceptor agonist. -
GC13822
(-)-JQ1
A selective inhibitor of BET bromodomains
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GN10445
(-)-pareruptorin A
-
GC90533
(-)-Pinoresinol
A lignan with diverse biological activities
-
GC70383
(-)-Vesamicol
(-)-Vesamicol (AH5183) is an inhibitor of acetylcholine transport into synaptic vesicles, with the IC50 of 75 nM.
-
GC73402
(16R)-Epothilone D
(16R)-KOS 862
(16R)-Epothilone D is the isomer of Epothilone D , and can be used as an experimental control. -
GC72769
(1R)-AZD-1480
(1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor.