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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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.
-
GC72832
(1R)-IDH889
(1R)-IDH889 is the isomer of IDH889 , and can be used as an experimental control.
-
GC70232
(1R,2R)-Calhex 231 hydrochloride
(1R,2R)-Calhex 231 hydrochloride is the isomer of Calhex 231 hydrochloride , and can be used as an experimental control.
-
GC70081
(1R,2R)-U-50488 hydrochloride
(1R,2R)-U-50488 hydrochloride is the absolute configuration of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a κ opioid receptor agonist.
-
GC67880
(1R,2S)-Xeruborbactam disodium
(1R,2S)-QPX7728 disodium
-
GC73081
(1R,3S)-Compound E
(1R,3S)-Compound E is the isomer of Compound E , and can be used as an experimental control.
-
GC73057
(1R,9R)-Exatecan mesylate
(1R,9R)-DX8951f
(1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate. -
GC70349
(1S)-CCR2 antagonist 1
(1S)-CCR2 antagonist 1 is a left-handed chiral body of CCR2 antagonist 1 .
-
GC73042
(1S,2S)-ML-SI3
(+)-trans-ML-SI3
(1S,2S)-ML-SI3 is a trans-isomer of ML-SI3 that targets all three isoforms of TRPML. -
GC65885
(1S,3R)-GNE-502
(1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor.
-
GC73056
(1S,9R)-Exatecan mesylate
(1S,9R)-DX8951f
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate. -
GC68525
(2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid
(2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid is a saponin that can be isolated from Rubus ellipticus var. obcordatus. It inhibits α-Glucosidase with an IC50 of 1.68 mM.
-
GC65777
(2-Pyridyldithio)-PEG2-Boc
(2-Pyridyldithio)-PEG2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC65623
(2-pyridyldithio)-PEG4 acid
(2-pyridyldithio)-PEG4 acid is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
-
GC65703
(2-Pyridyldithio)-PEG4-alcohol
(2-Pyridyldithio)-PEG4-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC11717
(24S)-MC 976
-
GC68509
(25R)-12α-Hydroxyspirost-4-en-3-one
(25R)-12α-Hydroxyspirost-4-en-3-one is a secondary metabolite produced by Nocardia globerula from Hecogenin.
-
GC70234
(2R)-Octyl-α-hydroxyglutarate sodium
(2R)-Octyl-α-hydroxyglutarate (sodium) is the sodium salt form of (2R)-Octyl-α-hydroxyglutarate.
-
GC70210
(2R)-SR59230A
(2R)-SR59230A is the isomer of SR59230A , and can be used as an experimental control.
-
GC73089
(2R)-Vildagliptin
(2R)-LAF237; (2R)-NVP-LAF 237
(2R)-Vildagliptin is the isomer of Vildagliptin , and can be used as an experimental control. -
GC73162
(2R,2R)-PF-07258669
(2R,2R)-PF-07258669 is a MC4R (melanocortin 4 receptor) antagonist.
-
GC70784
(2R,3R)-Firazorexton
(2R,3R)-Firazorexton ((2R,3R)-TAK-994 free base) is an isomer of Firazorexton .
-
GC73067
(2R,3R)-GSK973
(2R,3R)-GSK973 is an isomer of GSK973.
-
GC68522
(2R,3S)-Brassinazole
Brassinazole (0.5, 1, 5 μM) significantly caused morphological abnormalities in seedlings similar to BR-deficient mutants. Brassinazole resulted in dwarfism and altered leaf morphology, such as the typical downward curling and dark green appearance seen in Arabidopsis BR-deficient mutants. However, treatment with 10 nM BR reversed the dwarfism.
-
GC70605
(2R,4S)-Hydroxy Itraconazole-d5
(2R,4S)-Hydroxy Itraconazole-d5 is the deuterium labeled (2R,4S)-Hydroxy Itraconazole.
-
GC68524
(2S)-N3-IsoSer (DCHA)
"(2S)-N3-IsoSer DCHA" is a click chemistry reagent, which is a chiral α-hydroxy acid containing azide."
-
GC68523
(2S,3R)-Brassinazole
(2S,3R)-Brassinazole is an isomer of brassinazole, which is a compound that inhibits the biosynthesis of brassinosteroids (BR), a class of plant steroids, by acting on the oxidation process from 6-oxo-campestanol to teasterone. (2S,3R)-Brassinazole may be the most active form of brassinazole.
-
GC72621
(2S,3R,5S)-7-Deaza-2'-deoxy-7-iodoadenosine
(2S,3R,5S)-7-Deaza-2'-deoxy-7-iodoadenosine is the isomer of 7-Deaza-2'-deoxy-7-iodoadenosine , and can be used as an experimental control.
-
GC72663
(3E,8Z,11Z)-3,8,11-Tetradecatrienyl acetate
(3E,8Z,11Z)-3,8,11-Tetradecatrienyl acetate is a sex pheromone capable of attracting male South American tomato pinworms (Scrobipalpuloides absoluta), which can be isolated from the tomato pest.
-
GC73117
(3R,10R,14aS)-AZD4625
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 , and can be used as an experimental control.
-
GC72813
(3R,5R,6S)-Atogepant
(3R,5R,6S)-MK-8031; (3R,5R,6S)-AGN-241689
(3R,5R,6S)-Atogepant ((3R,5R,6S)-MK-8031) is the enantiomer of Atogepant. -
GC73214
(3S,4R)-GNE-6893
(3S,4R)-GNE-6893 is a potent and orally active HPK1 inhibitor.
-
GC74160
(3S,4S)-Tivantinib
(3S,4S)-ARQ 197; ARQ 198
(3S,4S)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. -
GC68317
(3S,5R)-Fluvastatin-d6 sodium
(3S,5R)-XU 62-320 D6
-
GC72936
(3S,5S,6R)-Navtemadlin
(3S,5S,6R)-AMG 232; (3S,5S,6R)-KRT-232
(3S,5S,6R)-Navtemadlin is the isomer of Navtemadlin , and can be used as an experimental control. -
GC73101
(4S)-PROTAC SOS1 degrader-1 diTFA
(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader.
-
GC68574
(6R)-ML753286
(6R)-ML753286 is an isomer of ML753286. ML753286 is an orally active and selective inhibitor of BCRP (breast cancer resistance protein), with an IC50 of 0.6 μM. ML753286 has high permeability and low to moderate clearance in rodent and human liver S9 fractions, and plasma stability across different species.
-
GC72962
(7R)-SBP-0636457
(7R)-SBI-0636457; (7R)-SB1-0636457
(7R)-SBP-0636457 is the isomer of SBP-0636457 , and can be used as an experimental control. -
GC73955
(7S)-BAY-593
(7S)-BAY-593 is the S-enantiomer of BAY-593.
-
GC73534
(9R,12aR)-AZD4747
(9R, 12aR)-AZD4747 is a diastereomer of AZD4747.
-
GC68652
(Aminooxy)acetamide-Val-Cit-PAB-MMAE
(Aminooxy)acetamide-Val-Cit-PAB-MMAE (MMAE 5) is an intermediate used in the synthesis and preparation of drug-conjugates for ADCs. It forms a MMAE polyamide conjugate by forming an oxime bond with a polyamide. The MMAE polyamide conjugate can then be linked to Trastuzumab to create an ADC.
-
GC52442
(D)-PPA 1 (trifluoroacetate salt)
DPPA-1, NYSKPTDRQYHF
An inhibitor of the PD-1-PD-L1 protein-protein interaction -
GC69009
(D)-PPA 1 TFA
(D)-PPA 1 TFA is an anti-hydrolysis D-peptide antagonist. It is an effective PD-1/PD-L1 inhibitor with an affinity of 0.51 μM for binding to PD-1, and it works both in vitro and in vivo.
-
GC15373
(E)-2-Decenoic acid
trans-2-Decylenic Acid
An unsaturated fatty acid found in royal jelly -
GC66255
(E)-3,4,5-Trimethoxycinnamic acid
TMCA
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy. -
GC72618
(E)-3,4-Dimethoxychalcone
(E)-3,4-Dimethoxychalcone is an isoform of 3,4-Dimethoxychalcone , a potential antimicrobial and antioxidant agent.
-
GC70220
(E)-Crotylbarbital
(E)-Crotylbarbital is the isomer of Crotylbarbital.
-
GC66371
(E)-Ferulic acid-d3
(E)-Coniferic acid-d3
(E)-Ferulic acid-d3 ((E)-Coniferic acid-d3) is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299. -
GC91418
(E)-KPT-330
KTP-330; trans Selinexor
(E)-KPT-330 is a metabolite of the exportin 1 (XPO1/CRM1) inhibitor selinexor. -
GC67663
(E)-TCO-PEG4-NHS ester
(E)-TCO-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
-
GC72591
(E,E)-RGFP966
(E,E)-RGFP966 is a selective and CNS permeable HDAC3 inhibitor that can be used for the research of Huntington’s disease.
-
GC25000
(E/Z)-BCI
BCI, NSC 150117
(E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells. -
GC91543
(E/Z)-Droloxifene
3-Hydroxytamoxifen
(E/Z)-Droloxifene is a mixture of (E)-droloxifene, a selective estrogen receptor modulator (SERM), and (Z)-droloxifene. -
GC72756
(E/Z)-Necrosulfonamide
(E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide.
-
GC67476
(E/Z)-Sulindac sulfide
(E/Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM). (E/Z)-Sulindac sulfide selectively reduces Aβ42 production in favor of shorter Aβ species. (E/Z)-Sulindac sulfide can be used for researching Alzheimer's disease.
-
GC72216
(Gly14)-Humanin (human) (acetate)
(Gly14)-Humanin (human) (14-Glycine-Humanin (human)) acetate is an analog of Humanin in which the 14th amino acid serine was replaced with glycine (Gly).
-
GA11210
(H-Cys-OH)2
(-)-Cystine, NSC 13203
-
GC72210
(Leu31,Pro34)-Peptide YY (human) (TFA)
(Leu31,Pro34)-Peptide YY (human) (TFA) is the TFA form of (Leu31,Pro34)-Peptide YY (human) .
-
GC72235
(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin acetate
(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist.
-
GC72195
(Pro3) GIP, human TFA
(Pro3) GIP, human TFA is an efficacious, stable and specifichuman GIP receptor (hGIPR)full agonist.
-
GN10783
(R) Ginsenoside Rh2
-
GC74692
(R)-(+)-Aminoglutethimide
d-Aminoglutethimide
(R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. -
GC69834
(R)-(+)-Dimethindene maleate
(R)-(+)-Dimethindene maleate is an orally active H1-receptor blocker with anti-histamine properties in pigs.
-
GC74261
(R)-(+)-O-Demethylbuchenavianine
(R)-(+)-O-Demetlbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK).
-
GC69823
(R)-(-)-Ibuprofen-d3
(R)-Ibuprofen-d3
(R)-(-)-Ibuprofen-d3 is the deuterated form of (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, which has no effect on COX and can inhibit NF-κB activation. (R)-(-)-Ibuprofen has anti-inflammatory properties and can be used in pain relief research.
-
GC91185
(R)-(-)-Metalaxyl-d6
An internal standard for the quantification of (R)-(−)-metalaxyl
-
GC91359
(R)-(4-Bromophenyl)(phenyl)methanamine
(R)-(4-Bromophenyl)(phenyl)methanamine is a synthetic intermediate.
-
GC91125
(R)-2-(3-(2-Ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxylic Acid
An intermediate in the synthesis of ervogastat
-
GC71626
(R)-3-Hydroxybutanoic acid-13C2 sodium
(R)-3-Hydroxybutanoic acid-13C2 (sodium) is the 13C labeled (R)-3-Hydroxybutanoic acid (sodium) .
-
GC69793
(R)-5-O-Benzoyl-1,2-di-O-isopropylidene-alpha-D-xylofuranose
(R)-5-O-Benzoyl-1,2-di-O-isopropylidene-alpha-D-xylofuranose is a purine nucleoside analogue. Purine nucleoside analogues have broad anti-tumor activity and target inert lymphoid malignancies. The anticancer mechanism in this process depends on inhibiting DNA synthesis, inducing apoptosis (cell death), etc.
-
GC66904
(R)-8-Azido-2-(Fmoc-amino)octanoic acid
(R)-8-Azido-2-(Fmoc-amino)octanoic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
-
GC91906
(R)-AS-1
(R)-AS-1 is a positive allosteric modulator of excitatory amino acid transporter 2 (EAAT2; EC50 = 11 nM in a glutamate uptake assay).
-
GC67688
(R)-Asundexian
(R)-BAY-2433334
-
GC25001
(R)-Avanafil
R-Avanafil is a strong competitive inhibitor of phosphodiesterase 5 (PDE5) with a demonstrated in vitro IC 50 of 5.2 nM.
-
GC73037
(R)-Benpyrine
(R)-Benpyrine is the isomer of Benpyrine , and can be used as an experimental control.
-
GC72968
(R)-BI-2852
(R)-BI-2852 is the isomer of BI-2852 , and can be used as an experimental control.
-
GC73749
(R)-Birabresib
(R)-OTX-015; (R)-MK-8628
(R)-Birabresib is the isomer of Birabresib , and can be used as an experimental control. -
GC69805
(R)-Casopitant
(R)-GW679769
(R)-Casopitant ((R)-GW679769) is an isomer of Casopitant. Casopitant is an NK(1) receptor antagonist that can be used in the research of chemotherapy-induced nausea and vomiting.
-
GC14729
(R)-Crizotinib
PF 2341066
A c-MET and ALK receptor tyrosine kinase inhibitor -
GC73545
(R)-DZD1516
(R)-DZD1516 is the R enantiomer of DZD1516.
-
GC69812
(R)-Elexacaftor
(R)-VX-445
(R)-Elexacaftor is the enantiomer of Elexacaftor (Compound 1) and comes from Compound 37 in patent WO2018107100A1. It is a corrector of cystic fibrosis transmembrane conductance regulator (CFTR), with an EC50 value of 0.29 uM for CFTR dF508.
-
GC67857
(R)-Elsubrutinib
(R)-ABBV-105
-
GC74127
(R)-Exatecan Intermediate 1
(R)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1.
-
GC70240
(R)-Fasiglifam
(R)-Fasiglifam is the isomer of Fasiglifam , and can be used as an experimental control.
-
GC73116
(R)-FT709
(R)-FT709 is an active compound.
-
GC70492
(R)-GDC-0927
(R)-GDC-0927 ((R)-SRN-927) is a (R)-enantiomer of GDC-0927 .
-
GC73737
(R)-GSK866
(R)-GSK866 is the (R)-enantiomer of GSK866.
-
GC70906
(R)-HH2853
(R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F.
-
GC52290
(R)-HTS-3
An inhibitor of LPCAT3
-
GC70609
(R)-IDO/TDO-IN-1
(R)-IDO/TDO-IN-1 (compound 25) is an indoleamine-2,3-dioxygenase (IDO) inhibitor, with good pharmacokinetic properties.
-
GC72833
(R)-INCB054329
(R)-INCB054329 is the isomer of INCB054329 , and can be used as an experimental control.
-
GC67864
(R)-Irsenontrine
(R)-E2027
-
GC70322
(R)-L 888607
(R)-L 888607 is the isomer of L 888607 , and can be used as an experimental control.
-
GC66419
(R)-Lercanidipine-d3 hydrochloride
(R)-lercanidipine D3 (hydrochloride) is a deuterium labeled (R)-Lercanidipine hydrochloride. (R)-Lercanidipine D3 (hydrochloride), the R-enantiomer of Lercanidipine, is a calcium channel blocker.
-
GC73528
(R)-M3913
(R)-M3913(compound C-155) is a enantiomer of M3913.
-
GC71217
(R)-mchm5U
(R)-mchm5U is a diastereomer of (S)-mchm5U .
-
GC70839
(R)-Merimepodib
(R)-Merimepodib is the isomer of Merimepodib , and can be used as an experimental control.
-
GC67937
(R)-Mirtazapine
(R)-Org3770; (R)-6-Azamianserin
-
GC70870
(R)-MK-5046
(R)-MK-5046 is the isomer of MK-5046 , and can be used as an experimental control.