Signaling Pathways
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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.
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Products Related to Signaling Pathways(40699)
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SJB2-043 analog is an inhibitor of OTUB1 and USP8 (IC50s = 0.17 and 0.28 nM, respectively) and a derivative of the USP1/UAF1 complex and SARS-CoV-2 PLPro inhibitor SJB2-043.
- GC92012MT-1207 (hydrochloride)Purity: >98.00%
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively.
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PKN3 inhibitor compound 16 is an inhibitor of serine/threonine protein kinase N3 (IC50 = 14 nM).
- GC92018N,N′-DiferuloylputrescineCAS: 42369-86-8Purity: >95.00%
N,N′-Diferuloylputrescine is a polyamine that has been found in Z. mays and has diverse biological activities.
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4-hydroxy Nonenal Glutathione-d3 (4-HNE-GSH-d3) is intended for use as an internal standard for the quantification of 4-HNE-GSH by GC- or LC-MS.
- GC92026D-Val-Leu-Lys-pNACAS: 63589-93-5Purity: >98.00%
D-Val-Leu-Lys-pNA is a colorimetric substrate for plasmin.
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UCM-05194 is an agonist of lysophosphatidic acid receptor 1 (LPA1).
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N-Lithocholyl-L-leucine is a bile acid conjugate composed of lithocholic acid and L-leucine.
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Debio 0123 is an inhibitor of the checkpoint kinase WEE1 (IC50 = 0.8 nM).
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GPX4 inhibitor 17 is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4) and an inducer of ferroptosis.
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MCL0020 is a melanocortin receptor 4 (MC4R) antagonist.
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JQKD82 is a prodrug form of KDM5-C49, an inhibitor of Jumonji AT-rich interactive domain 1A (JARID1A), also known as lysine-specific demethylase 5A (KDM5A).
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SGC0946 is an inhibitor of the non-SET domain-containing methyltransferase DOT1L (IC50 = 0.3 nM).
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9(10)-Nitrooleate is a mixture of the nitroalkene endogenous lipid signaling molecules 9-nitrooleate.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC92004 | DPTIP (hydrochloride) | 2361799-64-4 | >95.00% | |
DPTIP is an inhibitor of neutral sphingomyelinase 2 (nSMase2; IC50 = 30 nM). | ||||
| GC92010 | SJB2-043 analog (trifluoroacetate salt) | - | >95.00% | |
SJB2-043 analog is an inhibitor of OTUB1 and USP8 (IC50s = 0.17 and 0.28 nM, respectively) and a derivative of the USP1/UAF1 complex and SARS-CoV-2 PLPro inhibitor SJB2-043. | ||||
| GC92012 | MT-1207 (hydrochloride) | - | >98.00% | |
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. | ||||
| GC92014 | PKN3 Inhibitor Compound 16 | 2361545-75-5 | >98.00% | |
PKN3 inhibitor compound 16 is an inhibitor of serine/threonine protein kinase N3 (IC50 = 14 nM). | ||||
| GC92015 | WYneN | 3052492-38-0 | >95.00% | |
WYneN is a chemoselective probe for the detection of sulfenylated proteins in live cells. | ||||
| GC92016 | WYneO | 1648555-11-6 | >95.00% | |
WyneO is a probe for the detection of sulfenylated proteins. | ||||
| GC92018 | N,N′-Diferuloylputrescine | 42369-86-8 | >95.00% | |
N,N′-Diferuloylputrescine is a polyamine that has been found in Z. mays and has diverse biological activities. | ||||
| GC92019 | 1-Octadecyl-2-hydroxy-sn-glycero-3-phosphate (sodium salt) | - | >95.00% | |
1-Octadecyl-2-hydroxy-sn-glycero-3-phosphate (1-Octadecyl LPA) is a LPA analog containing stearyl alcohol at the sn-1 position. | ||||
| GC92022 | 4-hydroxy Nonenal Glutathione-d3 | - | >99.00% | |
4-hydroxy Nonenal Glutathione-d3 (4-HNE-GSH-d3) is intended for use as an internal standard for the quantification of 4-HNE-GSH by GC- or LC-MS. | ||||
| GC92023 | PTX80 | 2376297-69-5 | >95.00% | |
PTX80 is an antagonist of p62 (IC50 = 31.18 nM for the human receptor). | ||||
| GC92024 | BPN-01 | - | >90.00% | |
BPN-01 is a fluorescent probe for cancer cells. | ||||
| GC92026 | D-Val-Leu-Lys-pNA | 63589-93-5 | >98.00% | |
D-Val-Leu-Lys-pNA is a colorimetric substrate for plasmin. | ||||
| GC92028 | UCM-05194 (ammonium salt) | - | >95.00% | |
UCM-05194 is an agonist of lysophosphatidic acid receptor 1 (LPA1). | ||||
| GC92029 | N-Lithocholyl-L-Leucine | 2095154-73-5 | >95.00% | |
N-Lithocholyl-L-leucine is a bile acid conjugate composed of lithocholic acid and L-leucine. | ||||
| GC92030 | Debio 0123 (hydrochloride) | - | >98.00% | |
Debio 0123 is an inhibitor of the checkpoint kinase WEE1 (IC50 = 0.8 nM). | ||||
| GC92031 | GPX4 Inhibitor 17 | - | >98.00% | |
GPX4 inhibitor 17 is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4) and an inducer of ferroptosis. | ||||
| GC92033 | HPG1860 | 2226133-29-3 | >98.00% | |
HPG1860 is a farnesoid X receptor (FXR) agonist. | ||||
| GC92036 | MCL0020 (trifluoroacetate salt) | - | >98.00% | |
MCL0020 is a melanocortin receptor 4 (MC4R) antagonist. | ||||
| GC92037 | JQKD82 (hydrochloride) | 2863676-87-1 | >98.00% | |
JQKD82 is a prodrug form of KDM5-C49, an inhibitor of Jumonji AT-rich interactive domain 1A (JARID1A), also known as lysine-specific demethylase 5A (KDM5A). | ||||
| GC92039 | NO-Rosa5 | - | - | |
NO-Rosa5 is a photocontrollable nitric oxide (NO) donor for in cellulo and ex vivo use. | ||||
| GC92040 | SGC0946 (trifluoroacetate salt) | - | >98.00% | |
SGC0946 is an inhibitor of the non-SET domain-containing methyltransferase DOT1L (IC50 = 0.3 nM). | ||||
| GC92043 | 9(10)-Nitrooleate | 1092676-99-7 | >95.00% | |
9(10)-Nitrooleate is a mixture of the nitroalkene endogenous lipid signaling molecules 9-nitrooleate. | ||||
| GC92044 | H1L1A1B3 | 3097638-09-7 | >95.00% | |
H1L1A1B3 is an ionizable cationic lipid that has been used in combination with other lipids in the formation of LNPs for the delivery of circular RNA (circRNA) in vitro and in vivo. | ||||
| GC92048 | O12-D3-I3 | - | >95.00% | |
O12-D3-I3 is an ionizable cationic lipid (pKa = 6.39) that has been used in the generation of lipid nanoparticles (LNPs) for siRNA delivery in vitro and in vivo. | ||||
