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
-
GC73510
(S)-SKBG-1
(S)-SKBG-1 is an inactive and covalent NONO ligand, used for assay control.
-
GC73683
(S)-STX-478
(S)-STX-478 is the S-enantiomer of STX-478.
-
GC72828
(S)-Subasumstat
(S)-TAK-981
(S)-Subasumstat is the isomer of Subasumstat , and can be used as an experimental control. -
GC66064
(S)-Thalidomide
(S)-(-)-Thalidomide
(S)-Thalidomide ((S)-(-)-Thalidomide) is the S-enantiomer of Thalidomide. (S)-Thalidomide has immunomodulatory, anti-inflammatory, antiangiogenic and pro-apoptotic effects. (S)-Thalidomide induces teratogenic effects by binding to cereblon (CRBN) . -
GC73435
(S)-TNG260
(S)-TNG260 is an isomer of TNG260.
-
GC69977
(S)-Veliflapon
(S)-BAY X 1005; (S)-DG-031
(S)-Veliflapon ((S)-BAY X 1005) is an orally active leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP) inhibitor. It inhibits the formation of leukotriene B4 (LTB4) in rat, mouse, and human white blood cells with IC50 values of 0.026 μM, 0.039 μM, and 0.22 μM respectively. (S)-Veliflapon exhibits enantioselectivity in human whole blood.
-
GC69979
(S)-VQW-765
(S)-AQW-051
(S)-VQW-765 ((S)-AQW-051) is a partial agonist of the α7 nicotinic acetylcholine receptor (nAChR) with oral activity, selectivity and efficacy. It has potential applications in cognitive impairments associated with neurological diseases such as Alzheimer's disease or schizophrenia.
-
GC72758
(S,R)-S63845
(S,R)-S63845 is the isomer of S63845 , and can be used as an experimental control.
-
GC65883
(S,R)-WT IDH1 Inhibitor 2
GSK321
(S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers. -
GC73839
(S,R,R)-VBY-825
(S, R, R)-VBY-825 is the isomer of VBY-825 , and can be used as an experimental control.
-
GC69944
(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA
(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA is a synthetic E3 ligase ligand-linker conjugate containing the (S,R,S)-AHPC ligand, which can be used in PROTAC research.
-
GC69945
(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-PEG3-NH2 TFA
"(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-PEG3-NH2 TFA" is a synthetic E3 ligase ligand-linker conjugate, which includes a ligand based on (S,R,S)-AHPC and a three-unit PEG linker."
-
GC69946
(S,R,S)-AHPC-amido-C7-acid
(S,R,S)-AHPC-amido-C7-acid contains a VHL ligand for recruiting E3 ubiquitin ligases and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used for designing PROTACs.
-
GC69947
(S,R,S)-AHPC-C10-NHBoc
(S,R,S)-AHPC-C10-NHBoc is a synthetic E3 ligase ligand-linker conjugate, containing a VHL ligand based on (S,R,S)-AHPC and one linker. It can be used to synthesize targeted PROTACs for BET.
-
GC68352
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
-
GC69743
(S,R,S)-AHPC-C4-NH2 hydrochloride
VH032-C4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 28
(S,R,S)-AHPC-C4-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate, containing a VHL ligand based on (S,R,S)-AHPC and one linker. It is used for the synthesis of targeted PROTACs for EED.
-
GC69948
(S,R,S)-AHPC-CO-C9-acid
VH032-NH-CO-C9-acid
"(S,R,S)-AHPC-CO-C9-acid" is a ligand-linker complex of E3 ligase, which can be attached to the ligand of a protein to form a PROTAC."
-
GC69949
(S,R,S)-AHPC-isobutyl acetate-methanesulfonothioate-Me-C10-NH2 TFA
(Please note that this is a chemical name and may not have a direct translation into English) (Please also note that the use of chemicals should only be done by trained professionals in appropriate settings with proper safety measures.) (Please consult with a professional chemist for accurate information regarding this compound.) The (S,R,S)-AHPC-isobutyl acetate-methanesulfonothioate-Me-C10-NH2 TFA is part of PROTAC BRD4 Degrader-12.
-
GC67831
(S,R,S)-AHPC-Me-C10-Br
-
GC67729
(S,R,S)-AHPC-Me-C6-NH2
-
GC66630
(S,R,S)-AHPC-PEG2-acid
(S,R,S)-AHPC-PEG2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC73083
(S,S)-BMS-984923
(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923.
-
GC73104
(S,S)-CPI-1612
(S,S)-CPI-1612 is the isomer of CPI-1612 , and can be used as an experimental control.
-
GC67672
(S,S)-GNE 5729
-
GC67682
(S,S)-GSK321
-
GC73095
(S,S,R)-AHPC-C6-NH2 hydrochloride
(S,S,R)-AHPC-C6-NH2 drochloride is the drochloride salt form of (S,S,R)-AHPC-C6-NH2.
-
GC74175
(S,S,R,S,R)-Boc-Dap-NE
(S,S,R,S,R)-Boc-Dap-NE is an isomer of the dipeptide Boc-Dap-NE.
-
GC72938
(S,S,S)-AHPC-Boc
(S,S,S)-VH032-Boc
(S,S,S)-AHPC-Boc is the isomer of (S,R,S)-AHPC-Boc , and can be used as an experimental control. -
GC74174
(S,S,S,S,R)-Boc-Dap-NE
(S,S,S,S,R)-Boc-Dap-NE is the inactive isomer of Boc-Dap-NE , and can be used as an experimental control.
-
GC67761
(Z)-10-Hydroxynortriptyline-d3
-
GC73208
(Z)-JQ1-TCO
JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1 , an inhibitor of BET.
-
GC72798
(Z)-ONO 1301
(Z)-ONO-AP 500-02
(Z)-ONO 1301 is the isomer of ONO 1301 , and can be used as an experimental control. -
GC26181
(±)-Catechin
rel-Cianidanol; rel-Catechuic acid
(±) - Catechin (rel Xianidanol) is the racemate of Catechin.
-
GC11965
(±)-Huperzine A
Hup A, (-)-Selagine
A neuroprotective AChE inhibitor -
GC20027
(±)5(6)-DiHET MaxSpec® Standard
(±)5,6-DiHETrE
5(6)-DiHET is a fully racemic version of the enantiomeric forms biosynthesized from 5(6)-EET by epoxide hydrolases.
-
GC26151
(−)-Apomorphine (hydrochloride hydrate)
5,6,6aR,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol, monohydrochloride, hydrate
(-)-Apomorphine (hydrochloride hydrate) acts as a potent dopamine receptor agonist with a broad spectrum on all D1- and D2-like receptors (D1, D2S, D2L, D3, D4, D5). -
GC26094
(−)-Apomorphine (hydrochloride)
NSC 11442
-
GC74183
1'-epi Gemcitabine hydrochloride
1'-epi LY 188011 hydrochloride
1'-epi Gemcitabine drochloride is the isomer of Gemcitabine drochloride , and can be used as an experimental control. -
GC65729
1,1,1-Trifluoroethyl-PEG2-azide
1,1,1-Trifluoroethyl-PEG2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC65715
1,1,1-Trifluoroethyl-PEG2-propargyl
1,1,1-Trifluoroethyl-PEG2-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC66567
1,1,1-Trifluoroethyl-PEG4-alcohol
1,1,1-Trifluoroethyl-PEG4-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC67011
1,1,1-Trifluoroethyl-PEG4-amine
111-Trifluoroethyl-PEG4-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC67295
1,1,1-Trifluoroethyl-PEG4-aminooxy
1,1,1-Trifluoroethyl-PEG4-aminooxy is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC67595
1,1,1-Trifluoroethyl-PEG4-azide
111-Trifluoroethyl-PEG4-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC66971
1,1,1-Trifluoroethyl-PEG4-propargyl
1,1,1-Trifluoroethyl-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC65718
1,1,1-Trifluoroethyl-PEG4-Tos
1,1,1-Trifluoroethyl-PEG4-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC67833
1,1,3-Tribromoacetone
-
GC71868
1,2,3,19-Tetrahydroxy-12-ursen-28-oic acid
1,2,3,19-Tetrahydroxy-12-ursen-28-oic acid is a Triterpenoid that isolated from the plant of Agrimonia Pilosa with antimalarial and antidiabetic activities.
-
GC17055
1,2,3,4,5,6-Hexabromocyclohexane
Potently and directly inhibits JAK2 tyrosine kinase autophosphorylation, specifically inhibiting ligand-dependent JAK2 activation.
-
GC90942
1,2,3,4,6,7,8,9-Octachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC90936
1,2,3,4,6,7,8-Heptachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC90937
1,2,3,4,7,8,9-Heptachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC90938
1,2,3,4,7,8-Hexachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC71736
1,2,3,4-Tetrahydrobenzo[h]quinolin-3-ol
1,2,3,4-Tetrahydrobenzo[h]quinolin-3-ol is a biological material or organic compound that can be used in life science research.
-
GC90934
1,2,3,6,7,8-Hexachlorodibenzo-p-dioxin
A polychlorinated dibenzodioxin
-
GC90939
1,2,3,6,7,8-Hexachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC90940
1,2,3,7,8,9-Hexachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC90943
1,2,3,7,8-Pentachlorodibenzofuran
A dioxin-like polychlorinated dibenzofuran
-
GC92074
1,2,3-Trioleoyl Glycerol-d5
Glyceryl Trioleate-d5; TG(18:1/18:1/18:1)-d5; Triolein-d5
1,2,3-Trioleoyl glycerol-d5 is intended for use as an internal standard for the quantification of 1,2,3-trioleoyl glycerol by GC- or LC-MS. -
GC66452
1,2-Bis(3-(trifluoromethyl)phenyl)diselane
1,2-Bis(3-(trifluoromethyl)phenyl)diselane is an active compound and can be used for research.
-
GC90744
1,2-Dioleoyl-3(R)-trimethylammoniumpropane (chloride)
A cationic lipid
-
GC90745
1,2-Dioleoyl-3(S)-trimethylammoniumpropane (chloride)
A cationic lipid
-
GC68484
1,2-O-Isopropylidene-5-O-p-toluoyl-a-D-xylofuranose
1,2-O-Isopropylidene-5-O-p-toluoyl-a-D-xylofuranose is a purine nucleoside analogue. Purine nucleoside analogues have broad anti-tumor activity and target malignant tumors in the inert lymphatic system. The anticancer mechanism in this process depends on inhibiting DNA synthesis, inducing apoptosis (cell death), etc.
-
GC66949
1,3-bis(carboxyethoxy)-2,2-bis(carboxyethoxy)propane
1,3-bis(carboxyethoxy)-2,2-bis(carboxyethoxy)propane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC67054
1,3-Bis-aminooxy propane
1,3-Bis-aminooxy propane is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC67985
1,3-Oxazolidine-2-thione
-
GC68134
1,3-Propanesultam
1,1-Dioxoisothiazolidine
-
GC68486
1,4-Diaminobutane-d8 dihydrochloride
1,4-Diaminobutane-d8 dihydrochloride is the deuterium-substituted 1,4-Diaminobutane dihydrochloride, which is more stable and largely as tracer for quantitation during the drug development process.
-
GC67200
1,6-Bis(mesyloxy)hexane
16-Bismesyloxyhexane is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
-
GC71928
1,7-Bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one
1,7-Bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one is a potent nucleocapsid (N) protein inhibitor can be isolated from Curcuma kwangsiensis.
-
GC70586
1,7-Dimethyluric acid-d3
1,7-Dimethyluric acid-d3 is the deuterium labeled 1,7-Dimethyluric acid.
-
GC71294
1-(2-Deoxy-β-D-threo-pentofuranosyl)thymine
1-(2-Deoxy-β-D-threo-pentofuranosyl)thymine is a thymidine analog.
-
GC52356
1-1(Z)-Hexadecenyl-2-Arachidonoyl-sn-glycero-3-PC
1-1(Z)-Hexadecenyl-2-Arachidonoyl-sn-glycero-3-Phosphocholine, 1-1(Z)-Hexadecenyl-2-Arachidonoyl-sn-glycero-3-Phosphatidylcholine, 16:0p/20:4-PC, PC(P-16:0/20:4), C16(plasm)-20:4-PC, PlgPC 16:0/20:4
A plasmalogen -
GC90952
1-Aminoguanosine-3',5'-monophosphate (sodium salt)
A substrate for cGMP-dependent protein kinase
-
GN10317
1-Deoxynojirimycin
BAY-h-5955, D-1-Deoxynojirimycin, 1-DNJ, 1-dNM, Moranoline
-
GC74704
1-Ethenylpyrene
1-Vinylpyrene
1-Ethenylpyrene (1-Vinylpyrene) is an anti-chemical carcinogen that inhibits the formation of skin tumors initiated by either DMBA or Benzo[a]pyrene. -
GC67844
1-Fluoronaphthalene
-
GC26199
1-heptadecanoyl-2-hydroxy-sn-glycero-3-phosphocholine
-
GC68495
1-Hexadecanol-d4
1-Hexadecanol-d4 is the deuterated form of 1-hexadecanol. 1-Hexadecanol is a fatty alcohol, which is a hydrophobic substrate.
-
GC68496
1-Hexadecanol-d5
1-Hexadecanol-d5 is the deuterated form of 1-hexadecanol. 1-Hexadecanol is a fatty alcohol, which is a hydrophobic substrate.
-
GC72552
1-Hydroxypyrene-d9
1-Hydroxypyrene-d9 is the deuterium labeled 1-Hydroxypyrene.
-
GC25004
1-Iodoadamantane
Adamantyl iodide
1-Iodoadamantane (Adamantyl iodide) is a chemical. -
GC66557
1-Isothiocyanato-PEG3-azide
1-Isothiocyanato-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC65697
1-Isothiocyanato-PEG4-alcohol
1-Isothiocyanato-PEG4-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC90774
1-Linoleoyl Lysophosphatidic Acid (sodium salt)
A glycerophospholipid
-
GC72838
1-Methyladenosine-d3 hydrochloride
1-Metladenosine-d3 drochloride is the drochloride salt form of deuterium labeled 1-Metladenosine.
-
GC92019
1-Octadecyl-2-hydroxy-sn-glycero-3-phosphate (sodium salt)
LPA O-18:0; O-18:0 LPA; 1-Octadecyl-2-hydroxy-sn-glycero-3-PA; 1-Octadecyl LPA; 1-Octadecyl Lysophosphatidic Acid; 1-Oleyl LPA; 1-Oleyl Lysophosphatidic Acid; PA(O-18:0/0:0); 1-Stearyl-2-hydroxy-sn-glycero-3-PA
1-Octadecyl-2-hydroxy-sn-glycero-3-phosphate (1-Octadecyl LPA) is a LPA analog containing stearyl alcohol at the sn-1 position. -
GC74657
1-Octanol-d17
Octanol-d17
1-Octanol-d17 is the deuterium labeled 1-Octanol. -
GC92061
1-Palmitoyl-2-13(S)-HODE-sn-glycero-3-PC
1-Hexadecanoyl-2-13(S)-HODE-sn-glycero-3-Phosphocholine; 13(S)-Hydroxyoctadecadienoic Acid-PLPC; 1-Palmitoyl-2-13(S)-HODE-sn-glycero-3-Phosphocholine; 1-Palmitoyl-2-(13-hydroxy-cis-9,trans-11-octadecadienoyl)-L-3-phosphatidylcholine
1-Palmitoyl-2-13(S)-HODE-sn-glycero-3-PC is an oxidized phospholipid that contains palmitic acid and 13(S)-HODE at the sn-1 and sn-2 positions, respectively. -
GC68501
1-Palmitoyl-2-oleoyl-sn-glycerol
1-Palmitoyl-2-oleoyl-sn-glycerol is an endogenous metabolite and a major diacylglycerol in hypoxia-inducible factor (HIF)-1.
-
GC90829
1-Palmitoyl-2-Pyropheophorbide a-sn-glycero-3-PC
A phospholipid-porphyrin conjugate
-
GC90811
1-Palmitoyl-d9-2-Arachidonoyl-sn-glycero-3-PC
An internal standard for the quantification of 1-palmitoyl-2-arachidonoyl-sn-glycero-3-PC
-
GC68502
1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine
1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can be chosen as a model volatile compound for studying the molecular species of oxidized phosphatidylcholines. This method was applied to actual food samples, namely soybean lecithin.
-
GC25003
1-[(4R,5R)-4,5-Dihydroxy-L-ornithine]echinocandin B hydrochloride (1:1)
Anidulafungin Nucleus
1-[(4R,5R)-4,5-Dihydroxy-L-ornithine]-Echinocandin B Hydrochloride (Anidulafungin Nucleus) is used in the commercialization and late-stage development of a semisynthetic antifungal anidulafungin/D-fructose. -
GC91585
10α-hydroxy Naltrexone
10α-hydroxy Naltrexone is a derivative of the opioid antagonist naltrexone.
-
GC90363
10(11)-Cl-BBQ
A mixture that acts as an AhR agonist
-
GC66057
10,11-Dihydrocarbamazepine
10,11-Dihydrocarbamazepine is the active metabolite of Oxcarbazepine. 10,11-Dihydrocarbamazepine also is an intermediate. Oxcarbazepine is rapidly and almost completely converted to 10,11-Dihydrocarbamazepine with probable Anticonvulsant efficacy.
-
GC91581
10-(Phosphonooxy)-1-decanole
10-Hydroxydecyl dihydrogen phosphate,HDP
10-(Phosphonooxy)-1-decanole is a hydrolytic degradation product of 10-methacryloyloxydecyl dihydrogen phosphate-N-methylacryloyl glycine (MDP-NMGly) dental primers. -
GC91226
10-Chloroestra-1,4-diene-3,17-dione
A sterone ERα agonist
-
GC12954
10-DAB (10-Deacetylbaccatin)
NSC 251677
An inhibitor of microtubule assembly