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(1378)
- Chromatin/Epigenetics(17)
- Metabolism(421)
- 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(36)
- Angiogenesis(85)
- GPCR/G protein(3)
- Stem Cell(27)
- Membrane Transporter/Ion Channel(216)
- Cancer Biology(455)
- Endocrinology and Hormones(167)
- Neuroscience(463)
- Obesity, Appetite Control & Diabetes(8)
- Peptide Inhibitors and Substrate(1)
- Other Signal Transduction(140)
- Immunology/Inflammation(1113)
- Cardiovascular(63)
- Vitamin D Related(0)
- Antibody-drug Conjugate/ADC Related(0)
- PROTAC(274)
- Ox Stress Reagents(25)
- Others(4340)
- Antiparasitics(10)
- Toxins(88)
- Drug Derivative(141)
- OGA(1)
Products for Signaling Pathways
- Cat.No. Product Name Information
-
GC79783
(R)-Liquiritigenin
(R)-4',7-Dihydroxyflavanone
(R)-Liquiritigenin ((R)-4',7-Dihydroxyflavanone) is a MAO inhibitor that acts as an inhibitor of recombinant human MAO-A ( IC50 9.97 μM) and recombinant human MAO-B ( IC50 3.91 μM).
-
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.
-
GC80315
(R)-Mevalonic acid sodium
(R)-MVA sodium
(R) -Mevalonic acid ( (R) -MVA) sodium is an isomer of Mevalonic acid.
-
GC70870
(R)-MK-5046
(R)-MK-5046 is the isomer of MK-5046 , and can be used as an experimental control.
-
GC70581
(R)-ML375
(R)-ML375 ((R)-VU0483253) is an enantiomer of ML375 .
-
GC71036
(R)-MPH-220
(R)-MPH-220 is the R isomer of MPH-220 .
-
GC72915
(R)-MRT199665
(R)-MRT199665 is an isomer of MRT199665.
-
GC73092
(R)-Necrocide 1
(R)-Necrocide 1 (compound (R)-38) a potent anticancer agent.
-
GC68475
(R)-Nicardipine
(R)-YC-93 free base
-
GC79263
(R)-Octopamine
(R)-Octopamine is a Gs-coupled receptor agonist.
-
GC72961
(R)-OP-1074
(R)-OP-1074 is the isomer of OP-1074 , and can be used as an experimental control.
-
GC71634
(R)-Oxybutynin hydrochloride
(R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist.
-
GC80328
(R)-PAD-PF2
(R)-PAD-PF2 is an isomer of PAD-PF2.
-
GC72807
(R)-PI3Kδ-IN-15
(R)-PI3Kδ-IN-15 is the R-enantiomer of PI3Kδ-IN-15.
-
GC72939
(R)-PR-924
(R)-PR-924 is the isomer of PR-924 , and can be used as an experimental control.
-
GC68408
(R)-Praziquantel-d11
-
GC68383
(R)-Preclamol
(+)-3-PPP
-
GC72922
(R)-Prinomastat
(R)-AG3340; (R)-KB-R9896
(R)-Prinomastat ((R)-AG3340) is the R-isomer of Prinomastat (a MMP Inhibitor).
-
GC70848
(R)-Safinamide
(R)-Safinamide, the enantiomer of safinamide , can inhibit MAO-B with an IC50 value of 0.45 μM.
-
GC79434
(R)-SARM1-IN-5
(R)-SARM1-IN-5 is the (R)-enantiomer of SARM1-IN-5.
-
GC72753
(R)-SCH 546738
(R)-SCH 546738 is the R-isomer of SCH 546738.
-
GC73509
(R)-SKBG-1
(R)-SKBG-1 is an RNA-binding protein NONO inhibitor.
-
GC73187
(R)-Sortilin antagonist 1
(R)-Sortilin antagonist 1 is a sortilin antagonist that blocks the sortilin mediated apoptosis pathway by interfering with the binding of sortilin to its ligand pro-neurotrophin.
-
GC73312
(R)-STU104
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation.
-
GC69839
(R)-Tegoprazan
(R)-CJ-12420; (R)-RQ-00000004
(R)-Tegoprazan ((R)-CJ-12420; example 3) is a benzimidazole derivative and an effective inhibitor of gastric H+/K+-ATPase. Its IC50 for canine kidney Na+/K+-ATPase is 98 nM. (R)-Tegoprazan has potential in the research of gastrointestinal diseases.
-
GC70204
(R)-TTA-P2
(R)-TTA-P2 is the isomer of TTA-P2 , and can be used as an experimental control.
-
GC70934
(R)-Vanzacaftor
(R)-Vanzacaftor ((R)-VX-121) is a regulator of cystic fibrosis transmembrane conduction regulator (CFTR).
-
GC79504
(R)-Verapamil
Dexverapamil
(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil.
-
GC69847
(R)-VT104
(R)-VT104 is the R-enantiomer of VT104. The IC50 value of (R)-VT104 for firefly luciferase is 0.1-1 μμ. VT104 is an orally active pan-TEAD deacetylase inhibitor.
-
GC73082
(R)-VX-11e
(R)-VX-11e (Compound 1) is an ERK2 inhibitor.
-
GC80322
(R,R)-Alnodesertib
(R,R)-ART0380
(R,R)-ART0380 (Compound 38) is the enantiomer of ART0380.
-
GC78916
(R,R)-ATV2301
(R,R)-ATV2301 is the R,R isomer of ATV2301.
-
GC80856
(R,R)-Bexobrutideg
(R,R)-NX-5948; (R,R)-BTK-IN-24
(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg.
-
GC73054
(R,R)-CPI-1612
(R,R)-CPI-1612 is the isomer of CPI-1612 , and can be used as an experimental control.
-
GC80012
(R,R)-Cyclo(Pro-Val)
(R,R)-Cyclo(Pro-Val) is a trans (D-L) diastereoisomer of valyl-prolyl diketopiperazine (cyclic dipeptide) [1].
-
GC14145
(R,R)-Formoterol
(-)-Formoterol;Arformoterol;Formoterol
β2-selective adrenergic agonist
-
GC80321
(R,R)-MMP-1-IN-1
(R,R)-MMP-1-IN-1 is the R,R-enantiomer of MMP-1-IN-1.
-
GC72759
(R,R)-S63845
(R,R)-S63845 is the isomer of S63845 , and can be used as an experimental control.
-
GC69836
(R,R)-VVD-118313
(R,R)-VVD-118313 is an isomer of VVD-118313. VVD-118313 is a selective JAK1 inhibitor that can block JAK1-dependent phosphorylation and cytokine signaling. VVD-118313 can be used for cancer research.
-
GC79852
(R,S)-STT3A/B-IN-1
(R,S)-STT3A/B-IN-1 (compound 32), the racemate of STT3A/B-IN-1, is a STT3A/B inhibitor.
-
GC81349
(R,S)-YAP-TEAD-IN-2
(R,S)-YAP-TEAD-IN-2 is the racemic mixture of YAP-TEAD-IN-2.
-
GC72820
(R,S,R)-ML334
(R,S,R)-LH601A
(R,S,R)-ML334 is the isomer of ML334 , and can be used as an experimental control.
-
GC74173
(R,S,S,R,S)-Boc-Dap-NE
(R,S,S,R,S)-Boc-Dap-NE is the inactive isomer of Boc-Dap-NE , and can be used as an experimental control.
-
GC69837
(R/S)-Alicaforsen
(R/S)-ISIS-2302
(R/S)-Alicaforsen is the racemic form of Alicaforsen, which consists of both R and S configurations. Alicaforsen is a 20-base length antisense oligonucleotide that inhibits the production of ICAM-1, an important adhesion molecule involved in the migration and transport process of white blood cells to inflammatory sites.
-
GC71582
(Rac)-5-Hydroxymethyl Tolterodine hydrochloride
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively).
-
GC70292
(Rac)-AMG8379
(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379.
-
GC71831
(Rac)-Anemonin
(Rac)-Anemonin ((Rac)-Pulsatilla camphor) is the diastereoisomer of Anemonin .
-
GC74234
(Rac)-Apremilast
(Rac)-CC-10004
(Rac)-Apremilast ((Rac)-CC-10004) is the racemic mixture of Apremilast.
-
GC69794
(Rac)-Arnebin 1
(Rac)-β,β-Dimethylacrylalkannin; (Rac)-β,β-?Dimethylacrylshikonin
(Rac)-Arnebin 1 is the racemic form of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. These compounds are naphthoquinones isolated from plants in the Lithospermum genus, with β,β-Dimethylacrylshikonin exhibiting anti-tumor activity.
-
GC68414
(Rac)-Atropine-d3
(Rac)-Tropine tropate-d3; (Rac)-Hyoscyamine-d3
-
GC73029
(Rac)-Baxdrostat
(Rac)-CIN-107
(Rac)-Baxdrostat is the isomer of Baxdrostat , and can be used as an experimental control.
-
GC79563
(rac)-BDM88951
(rac)-BDM88951 is the racemate of BDM88951.
-
GC71593
(Rac)-Bepotastine besilate
(Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) , and can be used as an experimental control.
-
GC69795
(Rac)-BIO8898
(Rac)-BIO8898 is a CD40-CD154 co-stimulatory interaction inhibitor. (Rac)-BIO8898 inhibits the binding of CD154 to CD40-Ig, with an IC50 of 25 μM.
-
GC79104
(Rac)-Chem-0199
(Rac)-Chem-0199 is the racemic mixture of Chem-0199.
-
GC80037
(Rac)-Dihydrokaempferol
(Rac)-Dihydrokaempferol is a flavonoid compound.
-
GC78896
(Rac)-Emtricitabine S-oxide
(Rac)-Emtricitabine sulfoxide; (Rac)-Emtricitabine Degradant-III
(Rac)-Emtricitabine S-oxide ((Rac)-Emtricitabine sulfoxide; (Rac)-Emtricitabine Degradant-III) is Emtricitabine S-oxide racemic modification.
-
GC69796
(Rac)-Etavopivat
(Rac)-FT-4202
(Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat. Etavopivat is an orally active activator of red blood cell pyruvate kinase-R (PKR), which can be used for research on sickle cell disease and other hemoglobin disorders.
-
GC70206
(Rac)-Golgicide A
(Rac)-Golgicide A ((Rac)-GCA) is a racemate of Golgicide A.
-
GC73045
(Rac)-GSK-3484862
(Rac)-GSK-3484862 is the isomer of GSK-3484862 , and can be used as an experimental control.
-
GC72502
(Rac)-H-Thr-OMe hydrochloride
(Rac)-H-Thr-OMe hydrochloride is the isomer of H-Thr-OMe hydrochloride , and can be used as an experimental control.
-
GC73049
(Rac)-JBJ-04-125-02 acetate
(Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02.
-
GC72991
(Rac)-Lisaftoclax
(Rac)-APG-2575
(Rac)-Lisaftoclax ((Rac)-APG-2575) is a Bcl-2 inhibitor that can be uesd for hematologic malignancy research (CN112898295A).
-
GC80490
(Rac)-LRK-4189
(Rac)-LRK-4189 is the racemate of LRK-4189.
-
GC71577
(Rac)-LY341495
(Rac)-LY341495 is the isomer of LY341495 , and can be used as an experimental control.
-
GC73585
(Rac)-M826
(Rac)-M826 is the racemate of M826.
-
GC78978
(rac)-Mitiperstat
(rac)-AZD4831
(rac)-Mitiperstat ((rac)-AZD4831) is the racemic form of Mitiperstat.
-
GC71576
(Rac)-Moxifloxacin
(Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base) is the isoform of Moxifloxacin Hydrochloride , which is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
-
GC79410
(rac)-NDT-19795
(rac)-NDT-19795 is the racemate of NDT-19795.
-
GC80489
(rac)-Nerandomilast
(rac)-BI 1015550
(rac)-Nerandomilast ((rac)-BI 1015550) is a mixture of enantiomeric isomers of Nerandomilast, among which only the (R)-enantiomer (i.e., Nerandomilast ) has PDE4B inhibitory activity; the (S)-enantiomer (i.e., (S)-Nerandomilast ) is basically inactive.
-
GC71574
(Rac)-NNC 55-0396
(Rac)-NNC 55-0396 is the racemate of NNC 55-0396 .
-
GC71205
(Rac)-Reparixin
(Rac)-Reparixin is the isomer of Reparixin , and can be used as an experimental control.
-
GC71283
(Rac)-Rotigotine
(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine.
-
GC69797
(Rac)-SHIN2
(Rac)-SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor with a 1,4-dihydropyran[2,3-c]pyrazole structure. It is involved in folate or one-carbon metabolism pathways and prevents viral infections. SHMT1 and SHMT2 are cytosolic and/or mitochondrial isoforms of serine hydroxymethyltransferase respectively.
-
GC69798
(Rac)-SNC80
(Rac)-NIH 10815
(Rac)-SNC80 is the racemic form of SNC80. SNC80 (NIH 10815) is an effective and highly selective non-peptide delta-opioid receptor agonist with a Ki of 1.78 nM and IC50 of 2.73 nM. SNC80 has anti-nociceptive, anti-hyperalgesic, and antidepressant-like effects, and can be used in research on various types of headaches.
-
GC74162
(Rac)-Tivantinib
(Rac)-ARQ 197; (Rac)-ARQ 198
(Rac)-Tivantinib is the isomer of Tivantinib , and can be used as an experimental control.
-
GC79253
(Rac)-Ulotaront hydrochloride
(Rac)-SEP-363856 hydrochloride; (Rac)-SEP-856 hydrochloride
(Rac)-Ulotaront hydrochloride ((Rac)-SEP-363856 hydrochloride) is the racemate of Ulotaront hydrochloride.
-
GC69799
(Rac)-ZLc-002
(Rac)-ZLc-002 is an inhibitor that interacts with the binding protein between nNOS and nitric oxide synthase 1 (NOS1AP). It inhibits inflammatory pain and chemotherapy-induced neuropathic pain, and synergistically reduces tumor cell viability with Paclitaxel.
-
GC79590
(Rac)-δ-Viniferin
(Rac)-δ-Viniferin is a racemate of δ-Viniferin, an isomer of ε-Viniferin.
-
GC71532
(rel)-Eglumegad
(rel)-Eglumegad ((rel)-LY354740) is a relative configuration of Eglumegad .
-
GC73075
(rel)-ML-SI3
trans-ML-SI3
(rel)-ML-SI3 is one of the active ingredients of ML-SI3 (another component is (cis)-ML-SI3) that targets three isoforms of TRPML.
-
GC74166
(rel)-Tivantinib
(rel)-ARQ 197; (rel)-(3R,4R)-ARQ 198
(rel)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET.
-
GC79636
(RS)-Pantoic acid sodium monohydrate
(RS) -Pantoic acid sodium monohydrate is an intermediate in the phosphopantothenate biosynthesis pathway for the de novo synthesis of R-pantothenate (vitamin B5) from valine in plants and microorganisms.
-
GC72543
(S)-(+)-N-3-Benzylnirvanol
(S)-(+)-N-3-Benzylnirvanol is a drug used formetabolic regulation.
-
GC25002
(S)-(-)-α-Methylbenzylamine
(S)-(-)-α-Methylbenzylamine is a chiral auxiliary in the enantiodivergent synthesis of simple isoquinoline alkaloids.
-
GC74262
(S)-(-)-O-Demethylbuchenavianine
(S)-(-)-O-Demetlbuchenavianine (Compound (S)-(−)-1) is a flavonoidal alkaloids.
-
GC80033
(S)-3-Hydroxy-1,5-diphenylpentan-1-one
(S)-3-Hydroxy-1,5-diphenylpentan-1-one is a natural phenolic compound.
-
GC79596
(S)-4-Hydroxymephenytoin
(S) -4-Hydroxy mephenytoin is a metabolite derived from the stereoselective metabolism of mephenytoin.
-
GC79514
(S)-6-Methylnicotine
(S)-6-Methylnicotine is a nicotinic acetylcholine receptor ( nAChR ) agonist that exhibits agonistic activity on isolated guinea pig ileum.
-
GC80045
(S)-7-Hydroxywarfarin
(S)-7-Hydroxywarfarin is the S stereoisomer of 7-Hydroxywarfarin.
-
GC70334
(S)-ar-Curcumene
(S)-ar-Curcumene ((+)-alpha-Curcumene) is a natural compound.
-
GC70821
(S)-ARI-1
(S)-ARI-1 is an S-enantiomer of ARI-1.
-
GC73433
(S)-BAY 2965501
(S)-BAY 2965501 is the left-handed isomer of BAY 2965501.
-
GC70237
(S)-BAY 73-6691
(S)-BAY 73-6691 is the isomer of BAY 73-6691 , and can be used as an experimental control.
-
GC73666
(S)-Bexicaserin
(S)-Bexcaserin (compound 2) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related diseases.
-
GC73058
(S)-BRD9500
(S)-BRD9500 is the isomer of BRD9500 , and can be used as an experimental control.
-
GC79592
(S)-DSM1465
(S)-DSM1465 is a Plasmodium dihydroorotate dehydrogenase ( DHODH ) inhibitor.
-
GC78936
(S)-Edelfosine
(S)-ET-18-OCH3
(S)-Edelfosine ((S)-ET-18-OCH3) is the (S)-enantiomer of Edelfosine (ET-18-OCH3).