- Cyclosporin A (Cyclosporine A) is an immunosuppressant agent widely used in post-allogeneic organ transplant to reduce the activity of the immune system.
- X Jia, .et al. , J Hazard Mater, 2020, Jun 4;399:123034 PMID: 32544768
- Y Huang, .et al. , Experimental and Therapeutic Medicine, 2020, 20(2), 736-747 PMID: 32742319
- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
-
Ubiquitin ligase inducer
Lenalidomide is a derivative of thalidomide. In vitro, lenalidomide has three main activities: direct anti-tumor effect, inhibition of the micro environment support for tumor cells, and immunomodulatory role. It induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity.- Daniel A. Rauch, .et al. , Retrovirology, 2020, 17: 27 PMID: 32859220
- A Hayano, .et al. , Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Kumar R, .et al. , Mol Biol Rep, 2018, Oct 11 PMID: 30311125
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
-
-
TNF-alpha inhibitor
Pomalidomide is a derivative of thalidomide and acts as an immunomodulator. -
E3 ligase ligand-linker conjugate
Pomalidomide-PEG4-Ph-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology. -
Thalidomide-based Cereblon ligand
Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
-
PROTAC linker
NH2-C2-NH-Boc (PROTAC Linker 22) is a PROTAC linker, which refers to the alkyl chain composition.NH2-C2-NH-Boc can be used in the synthesis of a series of PROTACs. -
PROTAC linker
Cl-C6-PEG4-O-CH2COOH (PROTAC Linker 4) is a PROTAC linker can be used in the synthesis of chloroalkane-containing PROTACs (HaloPROTACs). -
PROTAC linker
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule HaloPROTAC that incorporates the VH032 based VHL ligand and 5-unit PEG linker. -
PROTAC linker
Pomalidomide-PEG4-C-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology. -
degrader
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1. -
Mcl-1 inhibitor
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM. -
ligand-linker conjugate
CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker. -
PROTAC linker
Dox-Ph-PEG1-Cl (PROTAC Linker 34) is a PROTAC linker, which refers to the PEG composition. Dox-Ph-PEG1-Cl can be used in the synthesis of a series of PROTACs. -
Lenalidomide-based Cereblon ligand
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs. -
VH032-based VHL ligand
VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). -
PROTAC linker
Boc-NH-C6-amido-C4-acid is a PROTAC linker, which refers to the alkyl/ether composition. Boc-NH-C6-amido-C4-acid can be used in the synthesis of a series of PROTACs. -
PEG PROTAC linker
PEG6-(CH2CO2H)2 is a PEG derivative containing two terminal carboxylic acid groups. The hydrophilic PEG spacer increases solubility in aqueous media. -
PROTAC linker
Boc-NH-PEG2-C2-amido-C4-acid (PROTAC Linker 30) is a PROTAC linker, which refers to the PEG composition. Boc-NH-PEG2-C2-amido-C4-acid can be used in the synthesis of a series of PROTACs. -
PROTAC linker
NH2-Ph-C4-acid-NH2-Me (PROTAC Linker 31) is a PROTAC linker, which refers to the Alkyl-Chain composition. NH2-Ph-C4-acid-NH2-Me can be used in the synthesis of a series of PROTACs. - PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
-
ABL inhibitor
SNIPER(ABL)-062, in which an ABL inhibitor is linked to a ligand of cIAP1 via a linker containing a variable polyethylene glycol (PEG) unit, shows a potent activity to degrade the BCR-ABL protein. -
FLT-3 ITD degrader
PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction. -
MDM2 degrader
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 has the potential to be a new class of anticancer agent.- Lingling Chen, .et al. , Biochem Pharmacol, 2024, Nov 29:232:116688 PMID: 39617210
-
PROTAC BET degrader
PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression. -
E3 ligase ligand-linker conjugate
(S,R,S)-AHPC-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology. -
E3 ligase ligand-linker conjugate
Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology. -
PROTAC linker
Bis-PEG1-C-PEG1-CH2COOH (PROTAC Linker 26) is a PROTAC linker, which refers to the PEG composition. Bis-PEG1-C-PEG1-CH2COOH can be used in the synthesis of a series of PROTACs. -
E3 ligase ligand-linker conjugate
Pomalidomide-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a PEG linker used in PROTAC technology. -
CRBN degrader
PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader. -
PROTAC linker
Bis-NH2-C1-PEG3 (PROTAC Linker 24) is a PROTAC linker, which refers to the alkyl/ether composition. Bis-NH2-C1-PEG3 can be used in the synthesis of a series of PROTACs. -
ERRa degrader
PROTAC ERRalpha Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader. -
ERRα Degrader
PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader. -
PROTAC linker
Phenol-amido-C1-PEG3-N3 (PROTAC Linker 21) is a PROTAC linker, which refers to the PEG composition. Phenol-amido-C1-PEG3-N3 can be used in the synthesis of a series of PROTACs. -
PROTAC linker
N3-PEG4-C2-NH2 (PROTAC Linker 20) is a polyethylene glycol (PEG)-based PROTAC linker. N3-PEG4-C2-NH2 can be used in the synthesis of a series of PROTACs.