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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GC71925
10-Hydroxyaloin A
10-10-Hydroxyaloin A is potent SARS-CoV-2 inhibitor.
-
GC52398
10-oxo-12(Z)-Octadecenoic Acid ethyl ester
10-keto-12Z-Octadecenoic Acid ethyl ester, 10-oxo-12-cis-Octadecenoic Acid ethyl ester
An ester form of 10-oxo-12(Z)-octadecenoic acid -
GC52428
10-oxo-12(Z)-Octadecenoic Acid-d5
10-keto-12Z-Octadecenoic Acid-d5, 10-oxo-12-cis-Octadecenoic Acid-d5
An internal standard for the quantification of 10-oxo-12(Z)-octadecenoic acid -
GC13863
10Panx
10Panx
A peptide inhibitor of PANX1 -
GC52423
10Panx (trifluoroacetate salt)
10Panx1, WRQAAFVDSY
A peptide inhibitor of PANX1 -
GC68204
11-Azidoundecanoic acid
-
GC66224
11-Maleimidoundecanoic acid
11-Maleimidoundecanoic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC73480
113-N16B
113-N16B is an ionizable cationic lipid used for the generation of lipid nanoparticles (LNPs).
-
GC52343
113-O12B
An ionizable cationic lipidoid
-
GC92076
119-23
119-23 is an ionizable cationic lipid that has been used in the generation of lipid nanoparticles (LNPs) for the delivery of mRNA in vivo.
-
GC91213
12β-Hydroxyisocholic Acid
A bile acid
-
GN10444
12-O-tetradecanoyl phorbol-13-acetate
PMA; TPA; Phorbol myristate acetate
A PKC activator
-
GC90652
12-oxo-9(Z)-Dodecenoic Acid
A metabolite of linoleic acid and linolenic acid
-
GC71326
12R-LOX-IN-2
12R-LOX-IN-2 (compound 7b) is an inhibitor of 12R-lipoxygenase (12R-LOX).
-
GC91073
13(Z)-Docosenoic Acid (sodium salt)
A 22-carbon monounsaturated fatty acid
-
GC68488
15-Azido-pentadecanoic acid
Azido Palmitic Acid
15-Azido-pentadecanoic acid is a chemical reagent containing an azide group. Azido Palmitic Acid can be used to identify and characterize post-translational palmitoylated proteins using a simple and robust two-step labeling and detection technique.
-
GC65988
16-Azidohexadecanoic acid
16-Azidohexadecanoic acid, a synthetic fatty acid, can be used as a modification marker for nucleotides and a molecular probe for fatty acid metabolism.
-
GC17557
17 alpha-propionate
CB-03-01
A peripherally selective androgen receptor antagonist -
GC68493
17α-Hydroxyprogesterone-d8
17-Hydroxyprogesterone-d8; 17-OHP-d8
17α-Hydroxyprogesterone-d8 is the deuterated form of 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-OHP) is an endogenous progestogen that serves as a chemical intermediate in the biosynthesis of other steroid hormones, including glucocorticoids, androgens, and estrogens.
-
GC91109
17β-Estradiol 3-O-Sulfate (sodium salt)
An inactive metabolite of 17β-estradiol
-
GC90945
17β-Estradiol-2,4,16,16-d4 3-sulfate (sodium salt)
An internal standard for the quantification of 17β-estradiol-3-sulfate
-
GC65870
17β-Estradiol-3-β-D-glucuronide-d3 sodium
17β-Estradiol-3-β-D-glucuronide-d3 sodium is the deuterium labeled 17β-Estradiol-3-β-D-glucuronide.
-
GC68494
17β-HSD1-IN-1
17β-HSD1-IN-1 (Compound 1) is a highly selective inhibitor of 17β-HSD1, with IC50 values of 5.6 and 3155 nM for inhibition of 17β-HSD1 and 17β-HSD2, respectively. It can be used for research on non-small cell lung cancer (NSCLC).
-
GC71338
17β-HSD10-IN-1
17β-HSD10-IN-1 (compound 9) is an orally active inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) with blood-brain permeability.
-
GC11720
17-AAG (KOS953)
BMS 722782, CP 127374, KOS 953, NSC 330507, Tanespimycin
17-AAG(Geldanamycin), a natural benzoquinone ansamycin antibiotic, is the first established inhibitor of Hsp90. -
GC17210
17-AAG Hydrochloride
Tanespimycin Hydrochloride;NSC 330507 Hydrochloride;CP 127374 Hydrochloride;17AAG Hydrochloride;17 AAG Hydrochloride
Hsp90 inhibitor,geldanamycin analogue -
GC68426
17a-Hydroxypregnenolone-d3
-
GC71042
18β-Glycyrrhetyl-3-O-sulfate
18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)) is a potent type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) inhibitor with an IC50 of 0.10 µM using rat kidney microsome.
-
GC71169
18-Azido-stearic acid
18-Azido-stearic acid is a click chemistry reagent containing an azide group.
-
GC91773
18-hydroxy Oleoyl Leucine-d7
18-hydroxy Oleoyl leucine-d7 is intended for use as an internal standard for the quantification of 18-hydroxy oleoyl leucine by GC- or LC-MS.
-
GC15623
1alpha, 25-Dihydroxy VD2-D6
-
GC72952
1E7-03
1E7-03, a low MW tetradroquinoline derivative targeting protein phosphatase-1, can inhibit HIV-1 transcription.
-
GC90584
1H,1H,2H,2H-Perfluorodecanesulfonic Acid
A polyfluoroalkyl substance
-
GC90585
1H,1H,2H,2H-Perfluorohexanesulfonic Acid
A polyfluoroalkyl substance
-
GC52216
1H,1H,2H,2H-Perfluorooctanesulfonic Acid
6:2 Fluorotelomer Sulfonate, 6:2 Fluorotelomer Sulfonic Acid, 6:2 FTS, 6:2 FTSA
A polyfluoroalkyl substance -
GC90815
2',3'-cyclic NADP+ (sodium salt)
A substrate for CNP
-
GC66890
2',3'-Dideoxy-5-iodocytidine
2',3'-Dideoxy-5-iodocytidine is used for gene sequencing can be used as an antibiotic. 2',3'-Dideoxy-5-iodocytidine is particular effective against Mycobacterium.
-
GC52501
2',3'-Dideoxyadenosine 5'-triphosphate (lithium salt)
ddATP
An inhibitor of reverse transcriptases and DNA polymerases -
GC90803
2',3'-Dideoxyadenosine-5'-O-triphosphate (sodium salt)
A reverse transcriptase inhibitor and an active metabolite of ddA and ddI
-
GC71982
2',4'-Dihydroxy-6'-Methoxyacetophenone
2',4'-Dihydroxy-6'-Methoxyacetophenone is a phenolic acetophenone from Artemisia annua.
-
GC67628
2',7'-Dichlorofluorescein
2',7'-Dichlorofluorescein acts as a fluorescent probe (Ex=496 nm and Em=525 nm) for reactive oxygen species (ROS) measurement.
-
GC90813
2'-deoxy NAD+ (sodium salt)
A TRPM2 agonist
-
GC67627
2'-Deoxy-5'-O-DMT-2'-fluorouridine
2'-Deoxy-5'-O-DMT-2'-fluorouridine, a nucleoside analogue, is a 5'-O-DMTr-5-FUDR derivative with potent anti-yellow fever (YFV) activity.
-
GC67328
2'-Deoxy-L-adenosine
2'-Deoxy-L-adenosine is an orally active synthon for modified oligodeoxyribonucleotides. 2'-Deoxy-L-adenosine is a potent, specific and selective inhibitor of the replication of hepatitis B virus (HBV) as well as the closely related duck and woodchuck hepatitis viruses (WHV).
-
GC73523
2'-Deoxy-N3-methylcytidine hydriodide
2’-Deoxy-N3-metlcytidine driodide is a purine nucleoside analog.
-
GC74092
2'-Deoxyguanosine-13C10
Deoxyguanosine-13C10; Guanine deoxyriboside-13C10
2'-Deoxyguanosine-13C10 (Deoxyguanosine-13C10; Guanine deoxyriboside-13C10) is 13C-labeled 2'-Deoxyguanosine. -
GC71729
2'-Deoxyguanosine-13C10,15N5 monohydrate
2'-Deoxyguanosine-13C10,15N5 (monohydrate) is the 13C and 15N labeled 2'-Deoxyguanosine monohydrate.
-
GC70730
2'-Ethyl Simvastatin
2'-Ethyl Simvastatin (compound 6) is a Mevinolin analog, with HMG-CoA reductase inhibition.
-
GC25010
2'-Hydroxy-2-methoxychalcone
2'-Hydroxy-2-methoxychalcone is a chemical.
-
GC66651
2'-O,4'-C-Methyleneadenosine
LNA-A
2'-O,4'-C-Methyleneadenosine (LNA-A) is a locked nucleic acid (LNA) and is also an adenosine analog. -
GC66654
2'-O,4'-C-Methylenecytidine
LNA-C(Bz)
2'-O,4'-C-Methylenecytidine (LNA-C(Bz)) is a bicyclic nucleoside analogue with fixed N-type conformation. 2'-O,4'-C-Methylenecytidine can be used to synthesize oligonucleotides. 2'-O,4'-C-Methylenecytidine forms duplexes with complementary DNA and RNA strands. -
GC66655
2'-O,4'-C-Methyleneguanosine
LNA-G
2′-O,4′-C-Methyleneguanosine (LNA-G) is a reverse guanine analogue, where LNA (locked nucleic acid) is a nucleic acid analogue. LNA modification can be used in a variety of applications such as effective binding affinity to complementary sequences and greater nuclease resistance than natural nucleotides, offering great potential for applications in disease diagnosis and research. LNA-G is also available via KOD DNA polymerase, which allows the integration of LNA-G nucleotides into the DNA strand. -
GC68521
2'-O-MB-cAMP sodium
2'-O-Monobutyryl cyclic AMP sodium
2'-O-MB-cAMP (2'-O-Monobutyryl cyclic AM) sodium is an active precursor of Cyclic AMP.
-
GC52183
2'-O-Methyl-5-methyluridine
2'-O-Methylribothymidine, 2'-O-Methylthymidine
-
GC66713
2'-O-MOE-5-Me-C(Bz)
2'-O-MOE-5-Me-C (Bz) is a nucleotide for the stereoselective synthesis of nucleoside alkyl phosphonates.
-
GC66657
2'-O-MOE-5-Me-rC
2'-O-MOE-5-Me-rC is an active compound. 2'-O-MOE-5-Me-rC can be used for oligonucleotide synthesis.
-
GC66091
2'-O-MOE-5-Me-rU
2'-O-MOE-5-Me-rU is an active compound. 2'-O-MOE-5-Me-rU can be used for oligonucleotide synthesis.
-
GC66656
2'-O-MOE-rC
2'-O-MOE-rC is a 2'-O-MOE modified nucleoside. 2'-O-MOE-rC can be used for synthesis of DNA.
-
GC66652
2'-O-MOE-U
2'-O-MOE-U is a phosphoramidite, can be used for oligonucleotide synthesis.
-
GC70652
2'MeO6MF
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.
-
GC67384
2′-Deoxy-β-L-uridine
2'-Deoxy-β-L-uridine is a nucledside analogue and a specific substrate for the viral enzyme, shows no stereospecificity against herpes simplex 1 (HSV1) thymidine kinase (TK). 2′-Deoxy-β-L-uridine exerts antiviral activity via the interation of 5'-triphosphates with the viral DNA polymerase.
-
GC90517
2,2'-Bisnaloxone
A potential impurity in commercial preparations of naloxone
-
GC90941
2,3,4,6,7,8-Hexachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC66487
2,3,4,6-Tetra-o-acetyl-alpha-galactosylpyranosyl bromide
2,3,4,6-Tetra-o-acetyl-alpha-galactosylpyranosyl bromide is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC90944
2,3,4,7,8-Pentachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC90818
2,3,7,8-Tetrachlorodibenzo-p-dioxin
A toxicant and an agonist of AhR
-
GC90819
2,3,7,8-Tetrachlorodibenzofuran
A polychlorinated dibenzofuran and dioxin
-
GC12258
2,3-DCPE hydrochloride
-
GC67743
2,3-Dihydroxyquinoxaline
-
GC90081
2,3-dinor-8-iso Prostaglandin F1α
An active metabolite of arachidonic acid and 8-iso PGF2α
-
GC70354
2,3-Diphosphoglyceric acid pentasodium
2,3-Diphosphoglyceric acid (2,3-DPG) pentasodium is an intermediate of the glycolytic pathway.
-
GC25006
2,4'-Dihydroxybenzophenone
2,4'-Dihydroxybenzophenone (DHBP) is an organic compound used for the synthesis of pharmaceutical agents.
-
GC68044
2,4,6-Trihydroxybenzaldehyde
-
GC68452
2,4,6-Triiodophenol
-
GC71530
2,4-D-13C6
2,4-D-13C6 is the 13C-labeled 2,4-D.
-
GC68234
2,4-Difluorobenzaldehyde
-
GC71311
2,4-Difluorophenylethynylcobalamin
2,4-Difluorophenylethynylcobalamin is a potential B12 antivitamin via binding to human B12 -processing enzyme CblC with high affinity (KD=130 nm).
-
GC68132
2,6-Dichloroquinone-4-chloroimide
-
GC66679
2,6-Dimethyl-L-tyrosine
Dmt
2,6-Dimethyl-L-tyrosine (Dmt) is a tyrosine derivative that enhances receptor affinity, functional bioactivity and in vivo analgesia of opioid peptides. -
GC91055
2,6-Xylidine-d6 (hydrochloride)
An Analytical Reference Standard
-
GC71909
2,7"-Phloroglucinol-6,6'-bieckol
2,7"-Phloroglucinol-6,6'-bieckol is an orally active dual α-amylase/α-glucosidase inhibitor with IC50 values of 6.94 μM and 23.35 μM respectively.
-
GC68512
2,7-Dichlorodihydrofluorescein
DCFH2
2,7-Dichlorodihydrofluorescein (DCFH2) is a non-fluorescent probe. 2,7-Dichlorodihydrofluorescein produces highly fluorescent 2',7'-dichlorofluorescein (DCF), which can be used for measuring reactive oxygen species.
-
GC66721
2-(2-(6-chlorohexyloxy)ethoxy)ethanamine hydrochloride
2-(2-(6-chlorohexyloxy)ethoxy)ethanamine (hydrochloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC68504
2-(2-Methylbenzamido)acetic acid-d7
2-(2-Methylbenzamido)acetic acid-d7 is the deuterated form of 2-(2-Methylbenzamido)acetic acid. 2-(2-Methylbenzamido)acetic acid is a metabolite that can be detected in urine.
-
GC66678
2-(3-Trifluoromethylphenyl)glycine hydrochloride
2-(3-Trifluoromethylphenyl)glycine hydrochloride is a precursor of substituted 2-acetamido-5-aryl-l, 2,4-triazolones. Substituted 2-acetamido-5-aryl-l, 2,4-triazolones are dual V1a/V2 receptor antagonists and can be used in cardiovascular disease research.
-
GC67619
2-(4-Biphenylyl)-5-phenyl-1,3,4-oxadiazole
2-(4-Biphenylyl)-5-phenyl-1,3,4-oxadiazole is a laser dyes with high photoluminescence (PL) quantum efficiency.
-
GC68093
2-(4-Chlorophenoxy)ethanol
-
GC66595
2-(Azido-PEG2-amido)-1,3-propandiol
2-(Azido-PEG2-amido)-13-propandiol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC66746
2-(Azido-PEG3-amido)-1,3-bis(carboxylethoxy)propane
2-Azido-PEG3-amido-13-biscarboxylethoxypropane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC66548
2-(Azido-PEG3-amido)-1,3-bis(NHS ester)
2-(Azido-PEG3-amido)-1,3-bis(NHS ester) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC67303
2-(Biotin-amido)-1,3-bis-(C1-PEG1-acid)
2-(Biotin-amido)-13-bis(carboxylethoxy)propane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC90442
2-(Chloromethyl)-3-(2-methylphenyl)quinazolin-4(3H)-one
An Analytical Reference Standard
-
GC91650
2-(Morpholin-4-yl)ethane-1-sulfonamide
4-Morpholineethanesulfonamide
2-(Morpholin-4-yl)ethane-1-sulfonamide is a byproduct in the synthesis of diazo compounds. -
GC66326
2-(Naphthalen-1-yl)-5-phenyloxazole
α-NPO
2-(Naphthalen-1-yl)-5-phenyloxazole (α-NPO) is an organic fluorescent dye. 2-(Naphthalen-1-yl)-5-phenyloxazole has a nitrogen atom in its structure that can interfere with the nitrogen content from the amination step. -
GC25008
2-Acetamidofluorene
2-AAF, 2-Acetaminofluorene, N-2-Fluorenylacetamide, N-Acetyl-2-aminofluorene
-
GC67087
2-Amino-1,3-bis(carboxylethoxy)propane
2-Amino-13-bis(carboxylethoxy)propane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC74106
2-Amino-1,3-bis(carboxylethoxy)propane hydrochloride
2-Amino-1,3-bis(carboxylethoxy)propane drochloride is a non-protein amino acid, sulfamic acid.
-
GC66717
2-Amino-2-(p-tolyl)acetic acid
2-Amino-2-(p-tolyl)acetic acid is used for optimizing azide skeleton, and is the intermediate in the synthesis of 1,3, 4-thiadiazole compounds. 1,3,4-thiadiazole compounds exhibit potential anti-cancer activity, and inhibit glutaminase (GLSI).
-
GC68195
2-Amino-5-methylthiophene-3-carbonitrile
-
GC73817
2-APQC
2-APQC is a SIRT3 activator with the Kd value of 2.756 μM.