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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GC70581
(R)-ML375
(R)-ML375 ((R)-VU0483253) is an enantiomer of ML375 .
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GC71036
(R)-MPH-220
(R)-MPH-220 is the R isomer of MPH-220 .
-
GC72915
(R)-MRT199665
(R)-MRT199665 is an isomer of MRT199665.
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GC73092
(R)-Necrocide 1
(R)-Necrocide 1 (compound (R)-38) a potent anticancer agent.
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GC68475
(R)-Nicardipine
(R)-YC-93 free base
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GC67767
(R)-Olacaftor
(R)-VX-440
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GC72961
(R)-OP-1074
(R)-OP-1074 is the isomer of OP-1074 , and can be used as an experimental control.
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GC71634
(R)-Oxybutynin hydrochloride
(R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist.
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GC67717
(R)-PF-04991532
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GC72807
(R)-PI3Kδ-IN-15
(R)-PI3Kδ-IN-15 is the R-enantiomer of PI3Kδ-IN-15.
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GC72939
(R)-PR-924
(R)-PR-924 is the isomer of PR-924 , and can be used as an experimental control.
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GC68408
(R)-Praziquantel-d11
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GC68383
(R)-Preclamol
(+)-3-PPP
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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.
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GC72753
(R)-SCH 546738
(R)-SCH 546738 is the R-isomer of SCH 546738.
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GC73509
(R)-SKBG-1
(R)-SKBG-1 is an RNA-binding protein NONO inhibitor.
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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.
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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.
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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.
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GC70204
(R)-TTA-P2
(R)-TTA-P2 is the isomer of TTA-P2 , and can be used as an experimental control.
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GC70934
(R)-Vanzacaftor
(R)-Vanzacaftor ((R)-VX-121) is a regulator of cystic fibrosis transmembrane conduction regulator (CFTR).
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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.
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GC73082
(R)-VX-11e
(R)-VX-11e (Compound 1) is an ERK2 inhibitor.
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GC65884
(R,1R)-Tenofovir amibufenamide
(R,1R)-HS-10234
(R,1R)-Tenofovir amibufenamide ((R,1R)-HS-10234) can be used for the purifying a tenofovir prodrug. Tynofovir (tenofovir) is a nucleoside acids reverse transcriptase inhibitors. -
GC73054
(R,R)-CPI-1612
(R,R)-CPI-1612 is the isomer of CPI-1612 , and can be used as an experimental control.
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GC14145
(R,R)-Formoterol
(-)-Formoterol;Arformoterol;Formoterol
β2-selective adrenergic agonist -
GC72759
(R,R)-S63845
(R,R)-S63845 is the isomer of S63845 , and can be used as an experimental control.
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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.
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GC52185
(R,S)-Anatabine-d4
(±)-Anatabine-d4
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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.
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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.
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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.
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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.
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GC68414
(Rac)-Atropine-d3
(Rac)-Tropine tropate-d3; (Rac)-Hyoscyamine-d3
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GC73029
(Rac)-Baxdrostat
(Rac)-CIN-107
(Rac)-Baxdrostat is the isomer of Baxdrostat , and can be used as an experimental control. -
GC71593
(Rac)-Bepotastine besilate
(Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) , and can be used as an experimental control.
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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.
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GC67993
(Rac)-Cotinine-d4
(±)-Cotinine-d4; (Rac)-NIH-10498-d4
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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.
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GC70206
(Rac)-Golgicide A
(Rac)-Golgicide A ((Rac)-GCA) is a racemate of Golgicide A.
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GC73045
(Rac)-GSK-3484862
(Rac)-GSK-3484862 is the isomer of GSK-3484862 , and can be used as an experimental control.
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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.
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GC73049
(Rac)-JBJ-04-125-02 acetate
(Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02.
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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). -
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.
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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.
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GC71574
(Rac)-NNC 55-0396
(Rac)-NNC 55-0396 is the racemate of NNC 55-0396 .
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GC66334
(Rac)-PF-184 hydrate
(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects.
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GC71205
(Rac)-Reparixin
(Rac)-Reparixin is the isomer of Reparixin , and can be used as an experimental control.
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GC71283
(Rac)-Rotigotine
(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine.
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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.
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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.
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GC74162
(Rac)-Tivantinib
(Rac)-ARQ 197; (Rac)-ARQ 198
(Rac)-Tivantinib is the isomer of Tivantinib , and can be used as an experimental control. -
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.
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GC71532
(rel)-Eglumegad
(rel)-Eglumegad ((rel)-LY354740) is a relative configuration of Eglumegad .
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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. -
GC72543
(S)-(+)-N-3-Benzylnirvanol
(S)-(+)-N-3-Benzylnirvanol is a drug used formetabolic regulation.
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GC25002
(S)-(-)-α-Methylbenzylamine
(S)-(-)-α-Methylbenzylamine is a chiral auxiliary in the enantiodivergent synthesis of simple isoquinoline alkaloids.
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GC74262
(S)-(-)-O-Demethylbuchenavianine
(S)-(-)-O-Demetlbuchenavianine (Compound (S)-(−)-1) is a flavonoidal alkaloids.
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GC66076
(S)-1-Benzylpyrrolidin-3-ol
(S)-1-Benzylpyrrolidin-3-ol (Compound 14) can be used to synthesis impurities of the anti-hypertensive drug Barnidipine hydrochloride (HY-107322).
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GC52192
(S)-4'-nitro-Blebbistatin
(-)-4'-nitro-Blebbistatin, p-nitro-Blebbistatin, para-nitro-Blebbistatin
(S)-4'-nitro-Blebbistatin is a non-cytotoxic, photostable, fluorescent and specific Myosin II inhibitor, usd in the study of the specific role of myosin II in physiological, developmental, and cell biological studies. -
GC70334
(S)-ar-Curcumene
(S)-ar-Curcumene ((+)-alpha-Curcumene) is a natural compound.
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GC70821
(S)-ARI-1
(S)-ARI-1 is an S-enantiomer of ARI-1.
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GC73433
(S)-BAY 2965501
(S)-BAY 2965501 is the left-handed isomer of BAY 2965501.
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GC70237
(S)-BAY 73-6691
(S)-BAY 73-6691 is the isomer of BAY 73-6691 , and can be used as an experimental control.
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GC73666
(S)-Bexicaserin
(S)-Bexcaserin (compound 2) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related diseases.
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GC73058
(S)-BRD9500
(S)-BRD9500 is the isomer of BRD9500 , and can be used as an experimental control.
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GC71271
(S)-FTY720-phosphonate
FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.
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GC65877
(S)-GFB-12811
(S)-GFB-12811 (compound 596) is a potent and selective CDK5 inhibitor, with an IC50 value less than 10 nM. (S)-GFB-12811 can be used in the research of cell cycle progression, neuronal development, tumorigenesis.
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GC70624
(S)-GLPG0974
(S)-GLPG0974 is the isomer of GLPG0974 , and can be used as an experimental control.
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GC73078
(S)-GSK-3685032
(S)-GSK-3685032 is the isomer of GSK-3685032 , and can be used as an experimental control.
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GC72866
(S)-GSK852
(S)-GSK852 is a diastereomer of GSK852.
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GC72836
(S)-Ibuprofen acyl-β-D-glucuronide
(S)-Ibuprofen glucuronide
(S)-Ibuprofen acyl-β-D-glucuronide ((S)-Ibuprofen glucuronide) is a compound used to study the metabolism and pharmacokinetics of S-ibuprofen, a non-steroidal anti-inflammatory drug. -
GC69890
(S)-Imlunestrant tosylate
(S)-LY-3484356 tosylate
(S)-Imlunestrant tosylate ((S)-LY-3484356) is the (S)-enantiomer of Imlunestrant. It can be used for cancer research.
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GC69891
(S)-Indoximod-d3
1-Methyl-L-tryptophan-d3; (S)-NLG-8189-d3
(S)-Indoximod-d3 is the deuterated form of (S)-Indoximod. (S)-Indoximod (1-Methyl-L-tryptophan) is an inhibitor of indoleamine 2,3-dioxygenase (IDO). (S)-Indoximod can be used for cancer research.
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GC69904
(S)-JDQ-443
(S)-NVP-JDQ443
(S)-JDQ-443 is an isomer of JDQ-443. JDQ-443 is an orally effective and selective covalent KRAS G12C inhibitor. JDQ-443 has anti-tumor activity.
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GC73762
(S)-LTGO-33
(S)-LTGO-33 is a small molecule inhibitor of voltage-gated sodium channel NaV1.8.
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GC65997
(S)-LY3177833 hydrate
(S)-LY3177833 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. (S)-LY3177833 hydrate shows broad in vitro anticancer activity.
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GC69914
(S)-Malic acid-d3
(S)-Hydroxybutanedioic acid-d3; (S)-E 296-d3
(S)-Malic acid-d3 is the deuterated form of (S)-Malic acid. (S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a naturally occurring dicarboxylic acid and a source of fruity sour taste, commonly used as a food additive.
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GC71218
(S)-mchm5U
(S)-mchm5U is a hydroxylated form of mcm5U, may be present in tRNA from the silkworm Bombyx mori.
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GC67989
(S)-Mirtazapine
(S)-Org3770; (S)-6-Azamianserin
-
GC68410
(S)-Mirtazapine-d3
(S)-Org3770 D3; (S)-6-Azamianserin D3
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GC68476
(S)-Nicardipine
(S)-YC-93 free base
-
GC70340
(S)-NIK SMI1
(S)-NIK SMI1 is the isomer of NIK SMI1 , and can be used as an experimental control.
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GC71642
(S)-Ofloxacin-d3
(S)-Ofloxacin-d3 is the deuterium labeled Levofloxacin.
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GC70925
(S)-Osanetant
(S)-Osanetant is the S-enantiomer of Osanetant.
-
GC70606
(S)-PF-04449613
(S)-PF-04449613 is the left-handed isomer of PF-04449613 .
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GC69941
(S)-Renzapride
(S)-BRL 24924
(S)-Renzapride ((S)-BRL 24924) is an isomer of Renzapride. Renzapride is a 5-HT4 receptor agonist with a Ki value of 115 nM. It also acts as an antagonist for the 5HT2b and 5HT3 receptors. Renzapride can be used in research on constipation-predominant irritable bowel syndrome (C-IBS).
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GC71007
(S)-Retosiban
(S)-Retosiban is the isomer of Retosiban , and can be used as an experimental control.
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GC70295
(S)-Ro 32-0432
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor.
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GC73372
(S)-Sabutoclax
(S)-BI-97C1
(S)-Sabutoclax ((S)-BI-97C1), an optically pure apogossypol derivative, is pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. -
GC73527
(S)-SAR131675
(S)-SAR131675 is the S-enantiomer of SAR131675 , a potent and selective VEGFR3 inhibitor and a click chemistry reagent.
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GC72905
(S)-Setastine
(S)-EGIS-2062 free acid; (S)-EGYT-2062 free acid
(S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent antagonist of H1 receptor-mediated responses.