Search Result
Results for "
E3 ligating enzyme
" in MCE Product Catalog:
1648
Inhibitors & Agonists
253
Biochemical Assay Reagents
92
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-128807
-
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E3 ligase Ligand 10
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
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-
- HY-129653
-
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E3 ligase Ligand 18
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
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-
- HY-128811
-
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E3 ligase Ligand 14
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
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- HY-43961
-
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E3 ligase Ligand 8
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
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- HY-128810
-
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E3 ligase Ligand 13
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
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-
- HY-128806
-
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E3 ligase Ligand 9
|
Ligands for E3 Ligase
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Cancer
|
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E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
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- HY-KT001
-
-
- HY-144983
-
-
- HY-144980
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-
- HY-144985
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-
- HY-N8096
-
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Raddeanoside R17
Pulchinenoside E3
|
Others
|
Inflammation/Immunology
|
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Raddeanoside R17 (Pulchinenoside E3) is a saponin compound that can be isolated from the root of Pulsatilla koreana. Raddeanoside R17 shows anti-inflammatory effects.
|
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- HY-126458
-
-
- HY-130270
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-
- HY-125906
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-
- HY-130521
-
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Pomalidomide-amido-PEG3-C2-NH2
Cereblon Ligand-Linker Conjugates 22; E3 ligase Ligand-Linker Conjugates 55
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
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- HY-128822
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-
- HY-128813A
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-
- HY-128815
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-
- HY-128816A
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-
- HY-128820
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-
- HY-128819
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-
- HY-128826
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-
- HY-128812A
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-
- HY-128813
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-
- HY-128824
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-
- HY-128812
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-
- HY-128817
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-
- HY-128825
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-
- HY-128823
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- HY-128818
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-
- HY-128821
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-
- HY-128816
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- HY-128814
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- HY-103612
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- HY-21930
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Pomalidomide-PEG4-C-COOH
Cereblon Ligand -Linker Conjugates 1; E3 Ligase Ligand-Linker Conjugates 1
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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.
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- HY-115560
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- HY-103615
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- HY-41549
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Pomalidomide-PEG4-Ph-NH2
Cereblon Ligand-Linker Conjugates 9; E3 Ligase Ligand-Linker Conjugates 2
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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.
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- HY-112617
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- HY-128716
-
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Pomalidomide-PEG3-C2-NH2
Cereblon Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 30
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-PEG3-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
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- HY-112599
-
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Pomalidomide-PEG4-C2-NH2
Cereblon Ligand-Linker Conjugates 8; E3 Ligase Ligand-Linker Conjugates 22
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-PEG4-C2-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.
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- HY-115560A
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- HY-125884
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- HY-107439
-
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Thalidomide-O-amido-C8-NH2
Cereblon Ligand-Linker Conjugates 2; E3 Ligase Ligand-Linker Conjugates 20
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
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- HY-107438
-
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Thalidomide-O-amido-C4-NH2
Cereblon Ligand-Linker Conjugates 6; E3 Ligase Ligand-Linker Conjugates 19
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
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- HY-111824
-
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VH032-thiol-C6-NH2
VHL Ligand-Linker Conjugates 14; E3 ligase Ligand-Linker Conjugates 29
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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VH032-thiol-C6-NH2 (VHL Ligand-Linker Conjugates 14) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
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- HY-112618
-
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Thalidomide-O-amido-C6-NH2
Cereblon Ligand-Linker Conjugates 11; E3 Ligase Ligand-Linker Conjugates 25
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-O-amido-C6-NH2 (Cereblon Ligand-Linker Conjugates 11), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
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- HY-128716B
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Pomalidomide-PEG3-C2-NH2 hydrochloride
Cereblon Ligand-Linker Conjugates 5 hydrochloride; E3 ligase Ligand-Linker Conjugates 30 hydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 5) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
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- HY-112078
-
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(S,R,S)-AHPC-Me
VHL ligand 2; E3 ligase Ligand 1A
|
Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
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- HY-103614
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Thalidomide-O-amido-C8-NH2 TFA
Cereblon Ligand -Linker Conjugates 2 TFA; E3 Ligase Ligand-Linker Conjugates 20 TFA
|
E3 Ligase Ligand-Linker Conjugates
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Others
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Thalidomide-O-amido-C8-NH2 TFA (Cereblon Ligand -Linker Conjugates 2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
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- HY-103613
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Thalidomide-O-amido-C4-NH2 TFA
Cereblon Ligand-Linker Conjugates 6 TFA; E3 ligase Ligand-Linker Conjugates 19 TFA
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E3 Ligase Ligand-Linker Conjugates
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Others
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Thalidomide-O-amido-C4-NH2 TFA (Cereblon Ligand-Linker Conjugates 6 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
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- HY-42424
-
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(S,R,S)-AHPC-Me hydrochloride
VHL ligand 2 hydrochloride; E3 ligase Ligand 1
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
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- HY-42424A
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(S,R,S)-AHPC-Me dihydrochloride
VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride
|
Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
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- HY-125846
-
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(S,R,S)-AHPC-PEG1-OTs
VH032-PEG1-OTs; VHL Ligand-Linker Conjugates 2; E3 ligase Ligand-Linker Conjugates 51
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG1-OTs is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.
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- HY-112618A
-
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Thalidomide-O-amido-C6-NH2 TFA
Cereblon Ligand-Linker Conjugates 11 TFA; E3 Ligase Ligand-Linker Conjugates 25 TFA
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-O-amido-C6-NH2 TFA (Cereblon Ligand-Linker Conjugates 11 TFA), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
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- HY-107440
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Thalidomide-O-amido-PEG3-C2-NH2
Cereblon Ligand-Linker Conjugates 3 ; E3 Ligase Ligand-Linker Conjugates 14
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
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- HY-112617A
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- HY-103611
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- HY-125883
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- HY-114176
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- HY-128832
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- HY-103599
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(S,R,S)-AHPC-PEG2-N3
VH032-PEG2-N3; VHL Ligand-Linker Conjugates 6; E3 ligase Ligand-Linker Conjugates 13
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in PROTAC technology.
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- HY-103604
-
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(S,R,S)-AHPC-PEG4-NH2 hydrochloride
VH032-PEG4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 4 hydrochloride; E3 ligase Ligand-Linker Conjugates 7
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
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- HY-103601
-
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(S,R,S)-AHPC-PEG4-N3
VH032-PEG4-N3; VHL Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 4
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E3 Ligase Ligand-Linker Conjugates
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Others
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(S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
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- HY-103600
-
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(S,R,S)-AHPC-PEG1-N3
VH032-PEG1-N3; VHL Ligand-Linker Conjugates 9; E3 ligase Ligand-Linker Conjugates 3
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG1-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.
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- HY-103598
-
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(S,R,S)-AHPC-PEG3-N3
VH032-PEG3-N3; VHL Ligand-Linker Conjugates 8; E3 ligase Ligand-Linker Conjugates 12
|
E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG3-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
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- HY-103602
-
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(S,R,S)-AHPC-PEG3-NH2 hydrochloride
VH032-PEG3-NH2 hydrochloride; VHL Ligand-Linker Conjugates 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 5
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
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- HY-103602A
-
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(S,R,S)-AHPC-PEG3-NH2
VH032-PEG3-NH2; VHL Ligand-Linker Conjugates 1; E3 ligase Ligand-Linker Conjugates 5 Free Base
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E3 Ligase Ligand-Linker Conjugates
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Cancer
|
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(S,R,S)-AHPC-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
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- HY-103604A
-
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(S,R,S)-AHPC-PEG4-NH2
VH032-PEG4-NH2; VHL Ligand-Linker Conjugates 4 ; E3 ligase Ligand-Linker Conjugates 7 Free Base
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
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- HY-130271
-
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(S,R,S)-AHPC-PEG5-COOH
VH032-PEG5-COOH; VHL Ligand-Linker Conjugates 16; E3 Ligase Ligand-Linker Conjugates 58
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 5-unit PEG linker used in PROTAC technology.
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- HY-128848
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- HY-112600
-
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- HY-103603
-
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(S,R,S)-AHPC-PEG2-NH2 hydrochloride
VH032-PEG2-NH2 hydrochloride; VHL Ligand-Linker Conjugates 3 hydrochloride; E3 ligase Ligand-Linker Conjugates 6
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG2-NH2 hydrochloride (VH032-PEG2-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
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- HY-112600A
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- HY-128716A
-
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Pomalidomide-PEG3-C2-NH2 TFA
Cereblon Ligand-Linker Conjugates 5 TFA; E3 ligase Ligand-Linker Conjugates 30 TFA
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-PEG3-C2-NH2 TFA (Cereblon Ligand-Linker Conjugates 5 (TFA)) is a synthetic E3 ligase ligand-linker conjugate comprising a Pomalidomide (HY-10984)-based cereblon ligand and a 3-unit PEG linker. Pomalidomide-PEG3-C2-NH2 TFA can be used for the synthesis of PROTACs.
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- HY-125843
-
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Pomalidomide-PEG1-C2-N3
Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-PEG1-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology. Pomalidomide-PEG1-C2-N3 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC50 of 2.1 nM.
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- HY-103603A
-
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(S,R,S)-AHPC-PEG2-NH2
VH032-PEG2-NH2 ; VHL Ligand-Linker Conjugates 3 ; E3 ligase Ligand-Linker Conjugates 6 Free Base
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG2-NH2 (VH032-PEG2-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
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- HY-103606
-
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(S,R,S)-AHPC-PEG6-C4-Cl
VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG6-C4-Cl is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG6-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
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- HY-148834
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- HY-103607
-
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(S,R,S)-AHPC-PEG2-C4-Cl
VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
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- HY-147192
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- HY-143346
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CCW16
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Others
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Cancer
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CCW16 is the covalent ligand for the E3 ubiquitin ligase RNF4. CCW16 can be used in the synthesis of protein degraders.
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- HY-103605
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(S,R,S)-AHPC-C6-PEG3-C4-Cl
VH032-C6-PEG3-C4-Cl; VHL Ligand-Linker Conjugates 12; E3 ligase Ligand-Linker Conjugates 8
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
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- HY-143715
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- HY-141431
-
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Cbl-b-IN-2
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E3 Ligase Ligand-Linker Conjugates
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Cancer
Inflammation/Immunology
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Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
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- HY-13296
-
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PYR-41
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E1/E2/E3 Enzyme
Apoptosis
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Cancer
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PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
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- HY-136156
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- HY-153215
-
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MEL24
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Others
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Cancer
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MEL24 is an Mdm2 E3 ligase inhibitor that reduces cell survival and increases sensitivity to DNA damaging agents in a p53-dependent manner for in vitro antitumor studies.
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- HY-133799
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- HY-44432
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- HY-149934
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- HY-129703B
-
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- HY-129703
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- HY-W062696
-
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- HY-129703A
-
-
- HY-130798
-
-
- HY-P3173
-
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Pullulanase
R-enzyme
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Endogenous Metabolite
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Others
|
|
Pullulanase (R-enzyme) is a starch debranching enzyme, is often used in biochemical studies. Pullulanase hydrolyses the α-1,6 glucosidic linkages in starch, amylopectin, pullulan, and related oligosaccharides. Pullulanase converts polysaccharide into small fermentative sugars during saccharification.
|
-
- HY-136772
-
-
- HY-138551A
-
-
- HY-130683
-
-
- HY-148556
-
-
- HY-133699
-
|
Pomalidomide-PEG4-COOH
|
Ligands for E3 Ligase
|
Others
|
|
Pomalidomide-PEG4-COOH is a E3 ligase ligand-linker conjugate. Pomalidomide-PEG4-COOH contains the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology (extracted from patent WO2017184995A1).
|
-
- HY-133484B
-
-
- HY-132998
-
|
HDAC6 degrader-1
|
PROTACs
|
Others
|
|
HDAC6 degrader-1 is a PROTAC that comprises a selective HDAC6 inhibitor Nexturastat A (Nex A) as the HDAC6 binder, a linker and a ligand for recruiting E3 ligase. HDAC6 degrader-1 induces significant degradation of HDAC6, exhibits excellent selectivity against other HDACs, and demonstrates efficient inhibition of cell proliferation.
|
-
- HY-139656
-
-
- HY-128808
-
|
cIAP1 ligand 1
E3 ligase Ligand 12
|
Ligands for E3 Ligase
|
Cancer
|
|
cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER.
|
-
- HY-128809
-
|
cIAP1 ligand 2
E3 ligase Ligand 11
|
Ligands for E3 Ligase
|
Cancer
|
|
cIAP1 ligand 2 is the LCL161 derivative based IAP ligand. cIAP1 ligand 2 can be connected to the ABL ligand for protein by a linker to form SNIPER.
|
-
- HY-100507
-
-
- HY-130682
-
-
- HY-43722
-
|
Lenalidomide-Br
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
|
-
- HY-132288
-
|
Pom-8PEG
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader.
|
-
- HY-128756
-
|
SIAIS178
|
PROTACs
Bcr-Abl
|
Cancer
|
|
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
|
-
- HY-131189
-
|
N-Boc-SBP-0636457-OH
|
Ligands for E3 Ligase
|
Cancer
|
|
N-Boc-SBP-0636457-OH, a ligand for E3 ubiquitin ligase, is used in the recruitment of IAP E3 ligases. N-Boc-SBP-0636457-OH can be connected to the ligand for Bcl-xL by a linker to form PROTAC Bcl-xL degrader-1 (HY-131188).
|
-
- HY-141797
-
|
MS33
|
Histone Methyltransferase
PROTACs
|
Cancer
|
|
MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia.
|
-
- HY-141448
-
|
NRX-2663
|
β-catenin
|
Cancer
|
|
NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC50 of 22.9 µM and a Kd of 54.8 nM.
|
-
- HY-138550A
-
-
- HY-141450
-
|
NRX-103095
|
β-catenin
|
Cancer
|
|
NRX-103095 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-103095 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC50 of 163 nM.
|
-
- HY-131295
-
-
- HY-130642
-
-
- HY-132938
-
-
- HY-139655
-
-
- HY-133046
-
|
VHL Ligand-Linker Conjugates 17
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader.
|
-
- HY-130499
-
|
ERRα Ligand-Linker Conjugates 1
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader.
|
-
- HY-41547
-
|
Thalidomide 4-fluoride
Cereblon ligand 4; E3 ligase Ligand 4
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966).
|
-
- HY-103597
-
|
Thalidomide-O-COOH
Cereblon ligand 3; E3 ligase Ligand 3
|
Ligands for E3 Ligase
|
Others
|
|
Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-103596
-
|
Thalidomide-4-OH
Cereblon ligand 2; E3 ligase Ligand 2
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-128837
-
|
Nutlin carboxylic acid
MDM2 ligand 1; E3 ligase Ligand 16
|
Ligands for E3 Ligase
|
Cancer
|
|
Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-101291
-
-
- HY-141449
-
|
NRX-103094
|
Molecular Glues
β-catenin
|
Cancer
|
|
NRX-103094 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-103094 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.
|
-
- HY-152859
-
|
Brigimadlin
BI 907828
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Brigimadlin (BI 907828) is an E3 ubiquitin-protein ligase MDM-2 inhibitor. Brigimadlin serves as an antineoplastic agent.
|
-
- HY-125905
-
|
VH032-cyclopropane-F
VHL ligand 3; E3 ligase Ligand 19
|
Ligands for E3 Ligase
|
Cancer
|
|
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 1 is a partial degrader of SMARCA2 and SMARCA4.
|
-
- HY-148142
-
-
- HY-148143
-
-
- HY-132858
-
-
- HY-10984
-
-
- HY-130815A
-
-
- HY-130815
-
-
- HY-139345
-
-
- HY-130295
-
-
- HY-138783
-
-
- HY-132939
-
-
- HY-130640
-
-
- HY-123967
-
|
RNF5 inhibitor inh-02
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research.
|
-
- HY-140844
-
-
- HY-141010
-
-
- HY-141014
-
-
- HY-131185
-
-
- HY-134983
-
-
- HY-111836
-
|
NRX-252114
|
Molecular Glues
β-catenin
|
Cancer
|
|
NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation.
|
-
- HY-129610
-
|
KB02-SLF
|
PROTACs
FKBP
|
Cancer
|
|
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.
|
-
- HY-138792
-
-
- HY-138783A
-
-
- HY-138773
-
-
- HY-131874
-
-
- HY-138790
-
-
- HY-141015
-
-
- HY-138775
-
-
- HY-138774
-
-
- HY-128846A
-
-
- HY-131876
-
-
- HY-138860
-
-
- HY-131880
-
-
- HY-131889
-
-
- HY-138791
-
-
- HY-140055
-
-
- HY-130814
-
|
Thalidomide-NH-C4-NH2 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader.
|
-
- HY-138771
-
-
- HY-138782
-
-
- HY-138778
-
-
- HY-138776
-
-
- HY-128846
-
-
- HY-138780
-
-
- HY-141010A
-
-
- HY-130950
-
-
- HY-138777
-
-
- HY-138772
-
-
- HY-130951
-
-
- HY-141887
-
-
- HY-138781
-
-
- HY-130269
-
|
β-Naphthoflavone-CH2-OH
β-NF-CH2-OH
|
Ligands for E3 Ligase
|
Cancer
|
|
β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
|
-
- HY-132208
-
-
- HY-138784
-
-
- HY-130965
-
-
- HY-138784A
-
-
- HY-131888A
-
-
- HY-141010B
-
-
- HY-138845A
-
-
- HY-130964B
-
-
- HY-112617B
-
-
- HY-129395
-
-
- HY-133484
-
-
- HY-138845
-
-
- HY-131888
-
-
- HY-128836
-
-
- HY-115446A
-
|
Lenalidomide-C4-NH2 hydrochloride
Cereblon ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively.
|
-
- HY-110287
-
|
Apcin
|
APC
|
Cancer
|
|
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis.
|
-
- HY-129776
-
|
K-Ras ligand-Linker Conjugate 2
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-129775
-
|
K-Ras ligand-Linker Conjugate 1
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-138642
-
|
Vepdegestrant
ARV-471
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
|
Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~2 nM.
|
-
- HY-10984S2
-
|
Pomalidomide-d4
CC-4047-d4
|
Molecular Glues
Ligands for E3 Ligase
Apoptosis
|
Cancer
|
|
Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
|
-
- HY-133816A
-
-
- HY-136162A
-
-
- HY-133485B
-
-
- HY-138847
-
-
- HY-133817
-
-
- HY-130949
-
-
- HY-138858A
-
-
- HY-134986
-
-
- HY-138848A
-
-
- HY-133817A
-
-
- HY-130948
-
-
- HY-138787
-
-
- HY-133816
-
-
- HY-138859
-
-
- HY-131867
-
-
- HY-138789
-
-
- HY-138848
-
-
- HY-138846A
-
-
- HY-138858
-
-
- HY-136237
-
-
- HY-130963
-
-
- HY-138847A
-
-
- HY-129704B
-
-
- HY-135250
-
-
- HY-138846
-
-
- HY-133485
-
-
- HY-10984S
-
|
Pomalidomide-d5
CC-4047-d5
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Cancer
|
|
Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
|
-
- HY-134985
-
-
- HY-129704
-
-
- HY-136162
-
-
- HY-138788
-
-
- HY-138859A
-
-
- HY-139999
-
|
LCL-PEG3-N3
|
Ligands for E3 Ligase
|
Cancer
|
|
LCL-PEG3-N3 is a decoy oligonucleotide ligand for E3 ligase which can be used for developing chimeric molecules LCL-ER(dec), degrading the estrogen receptor.
|
-
- HY-123937
-
|
THAL-SNS-032
|
PROTACs
CDK
|
Cancer
|
|
THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
|
-
- HY-138853
-
-
- HY-130845
-
-
- HY-137538
-
-
- HY-138789A
-
-
- HY-138849A
-
-
- HY-129704A
-
-
- HY-134984A
-
-
- HY-139999A
-
-
- HY-134984
-
-
- HY-138850A
-
-
- HY-138850
-
-
- HY-138851
-
-
- HY-131998
-
-
- HY-138852
-
-
- HY-136161
-
-
- HY-130639
-
-
- HY-137537
-
-
- HY-138853A
-
-
- HY-128767
-
-
- HY-138851A
-
-
- HY-141423
-
-
- HY-138849
-
-
- HY-138852A
-
-
- HY-138788A
-
-
- HY-130991
-
|
K-Ras ligand-Linker Conjugate 6
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-147373
-
|
DA-PROTAC
|
PROTACs
Ligands for E3 Ligase
|
Cancer
|
|
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research.
|
-
- HY-138786
-
-
- HY-N0170
-
-
- HY-107438A
-
-
- HY-136166
-
-
- HY-130948B
-
-
- HY-107439A
-
-
- HY-112618B
-
-
- HY-122694
-
-
- HY-138786A
-
-
- HY-141423A
-
-
- HY-15694
-
|
SMIP004
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
|
-
- HY-138785A
-
-
- HY-130845A
-
-
- HY-138785
-
-
- HY-130816
-
|
(S,R,S)-AHPC-O-Ph-PEG1-NH2
VH032-O-Ph-PEG1-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02.
|
-
- HY-129917
-
|
KB02-JQ1
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
|
-
- HY-135250B
-
-
- HY-10984S1
-
|
Pomalidomide-d3
CC-4047-d3
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Cancer
|
|
Pomalidomide-d3 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors[1][2].
|
-
- HY-122694A
-
-
- HY-148130
-
|
Rugonersen
RG6091; RO7248824
|
E1/E2/E3 Enzyme
|
Others
|
|
Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch.
|
-
- HY-130716
-
-
- HY-138862
-
-
- HY-141432
-
|
Cbl-b-IN-3
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Cbl-b-IN-3 (Compound 23) is a casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 of < 1 nM. Cbl-b is an E3 ubiquitin ligase that negatively regulates T-cell activation.
|
-
- HY-131232
-
-
- HY-136163A
-
-
- HY-111760
-
|
NRX-252262
|
Molecular Glues
β-catenin
|
Cancer
|
|
NRX-252262 is a potent enhancer of the interaction between β-Catenin, and its cognate E3 ligase, SCF β-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM.
|
-
- HY-153357
-
|
NRX-0492
|
Btk
|
Cancer
|
|
NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex.
|
-
- HY-138856A
-
-
- HY-136163
-
-
- HY-138856
-
-
- HY-138854A
-
-
- HY-112599B
-
-
- HY-138855A
-
-
- HY-122710
-
-
- HY-135844
-
|
LS-102
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment.
|
-
- HY-136183
-
-
- HY-108372
-
|
Boc-C5-O-C5-O-C6-Cl
PROTAC Linker 2
|
PROTAC Linkers
|
Cancer
|
|
Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
|
-
- HY-137531
-
-
- HY-138854
-
-
- HY-138855
-
-
- HY-138857A
-
-
- HY-138857
-
-
- HY-131308
-
-
- HY-114176B
-
-
- HY-133144
-
|
Lenalidomide-OH
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
|
-
- HY-122710A
-
-
- HY-146237
-
|
Golcadomide
CC-99282
|
Ligands for E3 Ligase
Molecular Glues
|
Cancer
|
|
Golcadomide (CC-99282) is a potent and orally active cereblon (CRBN) E3 ligase modulator (CELMoD). Golcadomide co-opts CRBN to induce potent and targeted degradation of Ikaros and Aiolos. Golcadomide can be used for researching non-Hodgkin lymphomas.
|
-
- HY-128842
-
-
- HY-128843
-
-
- HY-128840
-
-
- HY-128841
-
-
- HY-138861A
-
-
- HY-148671
-
-
- HY-114176A
-
-
- HY-138861
-
-
- HY-A0003B
-
|
Lenalidomide hemihydrate
CC-5013 hemihydrate
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Cancer
|
|
Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-46531
-
-
- HY-A0003
-
|
Lenalidomide
CC-5013
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-A0003A
-
|
Lenalidomide hydrochloride
CC-5013 hydrochloride
|
Ligands for E3 Ligase
Molecular Glues
|
Cancer
Inflammation/Immunology
|
|
Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-145818
-
|
JPS035
|
HDAC
PROTACs
|
Cancer
|
|
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
|
-
- HY-145816
-
|
JPS016
|
HDAC
PROTACs
|
Cancer
|
|
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
|
-
- HY-145819
-
|
JPS036
|
HDAC
PROTACs
|
Cancer
|
|
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
|
-
- HY-145815
-
|
JPS014
|
HDAC
PROTACs
|
Cancer
|
|
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
|
-
- HY-44148
-
-
- HY-148406
-
-
- HY-136165
-
-
- HY-135250A
-
-
- HY-129523
-
|
PROTAC K-Ras Degrader-1
|
PROTACs
Ras
|
Cancer
|
|
PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades K-Ras based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-130988A
-
-
- HY-E70080
-
|
Vaccinia virus capping enzyme
|
Biochemical Assay Reagents
|
Others
|
|
Vaccinia virus capping enzyme is a transcription initiation factor. Vaccinia virus capping enzyme is a heterodimer of D1 (844 aa) and D12 (287 aa) polypeptides that executes all three steps in m7GpppRNA synthesis. Vaccinia virus capping enzyme has been used widely as a reagent for capping and cap-labeling RNAs in vitro.
|
-
- HY-130800
-
-
- HY-131959
-
-
- HY-131872
-
-
- HY-131912
-
-
- HY-136160
-
-
- HY-144841
-
|
Cemsidomide
CFT7455
|
Ligands for E3 Ligase
|
Cancer
|
|
Cemsidomide (CFT7455) is an orally active zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3) degrader. Cemsidomide is an anti-cancer agent that binds with high affinity to the cereblon E3 ligase (Kd of 0.9 nM) (WO2022032132A1; Compound 1).
|
-
- HY-131318
-
|
Lenalidomide-I
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609).
|
-
- HY-136688
-
|
MI-389
|
PROTACs
|
Cancer
|
|
MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4 CRBN E3 ligase.
|
-
- HY-130648
-
-
- HY-107440A
-
-
- HY-130835
-
|
FKBP12 PROTAC RC32
RC32
|
PROTACs
FKBP
|
Cancer
|
|
FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an Cereblon E3 ubiquitin ligase (Pomalidomide; HY-10984).
|
-
- HY-130297
-
|
PROTAC BCR-ABL1 ligand 1
|
Bcr-Abl
|
Cancer
|
|
PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.
|
-
- HY-134591
-
-
- HY-122702
-
|
PEG6-(CH2CO2H)2
|
PROTAC Linkers
|
Others
|
|
PEG6-(CH2CO2H)2 is a symmetric PEG PROTAC linker, for the synthesis of Homo-PROTACs which is bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.
|
-
- HY-131190
-
-
- HY-132992
-
-
- HY-130737
-
-
- HY-131646
-
-
- HY-130638
-
-
- HY-131647
-
-
- HY-14658
-
-
- HY-69220
-
|
7-Octynoic acid
|
PROTAC Linkers
|
Cancer
|
|
7-Octynoic acid (compound 42) is a PROTAC linker and can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-110204
-
|
Heclin
|
E1/E2/E3 Enzyme
|
Others
|
|
Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits several HECT ligases in tissue culture cells (IC50s=6.8, 6.3, and 6.9 μM for Smurf2, Nedd4, and WWP1 HECT ligase domains, respectively).
|
-
- HY-130849
-
-
- HY-131186
-
-
- HY-114324
-
|
PROTAC PARP1 degrader
|
PROTACs
PARP
|
Cancer
|
|
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
|
-
- HY-136006B
-
-
- HY-136186
-
-
- HY-123844
-
|
dBET57
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 Cereblon E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2.
|
-
- HY-112811
-
|
PROTAC CDK9 degrader-2
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC.
|
-
- HY-14658S
-
-
- HY-130711B
-
-
- HY-136008
-
-
- HY-133487A
-
-
- HY-145615
-
-
- HY-133139
-
-
- HY-129941
-
-
- HY-129941A
-
-
- HY-133020
-
|
ARD-266
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-108705
-
|
BI-3802
|
Molecular Glues
Bcl-2 Family
|
Cancer
|
|
BI-3802 is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity.
|
-
- HY-130713
-
-
- HY-133138
-
-
- HY-112098
-
|
PROTAC ERα Degrader-1
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
|
-
- HY-130847
-
-
- HY-103608
-
|
(S,R,S)-AHPC-(C3-PEG)2-C6-Cl
VHL Ligand-Linker Conjugates 11; E3 ligase Ligand-Linker Conjugates 11
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-(C3-PEG)2-C6-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-PEG)2-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-P2983
-
-
- HY-136184
-
-
- HY-141486
-
|
(Rac)-PROTAC PARP/EGFR ligand 1
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP.
|
-
- HY-125834
-
|
GMB-475
|
PROTACs
Bcr-Abl
Apoptosis
|
Cancer
|
|
GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent agent resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
|
-
- HY-129652
-
|
Halo PROTAC 1
|
AUTACs
|
Cancer
|
|
Halo PROTAC 1 is a conjugate of ligands for E3 and 22-atom-length linker. The connector of linker is Halogen group. Halo PROTAC 1 is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker. Halo PROTAC 1 can be uesd for the synthesis of AUTAC.
|
-
- HY-136187
-
-
- HY-108374
-
|
4-Azidobutylamine
|
PROTAC Linkers
|
Cancer
|
|
4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-131385
-
|
KB02-COOH
|
Ligands for E3 Ligase
|
Cancer
|
|
KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 (HY-129917) and KB02-SLF (HY-129610).
|
-
- HY-103603B
-
-
- HY-130988
-
|
Ipatasertib-NH2
GDC-0068-NH2; RG7440-NH2
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
|
-
- HY-136008A
-
-
- HY-130854
-
|
Thalidomide-NH-C6-NH-Boc
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).
|
-
- HY-130256
-
|
β-NF-JQ1
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
|
-
- HY-132296
-
|
GSK215
|
FAK
PROTACs
|
Cancer
|
|
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
|
-
- HY-130853
-
|
Thalidomide-NH-PEG2-C2-NH-Boc
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology.
|
-
- HY-131188
-
|
PROTAC Bcl-xL degrader-1
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively.
|
-
- HY-145479
-
|
PROTAC AR-V7 degrader-1
|
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM.
|
-
- HY-129774
-
|
Phthalimide-PEG4-MPDM-OH
|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG4-MPDM-OH is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-MPDM-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-130617
-
|
Pomalidomide-amido-C1-Br
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity.
|
-
- HY-130982
-
|
Lenalidomide-PEG3-iodine
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-PEG3-iodine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a 3-unit PEG linker. Lenalidomide-PEG3-iodine can be used in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
|
-
- HY-100972
-
|
ARV-771
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
|
-
- HY-130715
-
|
tert-Butyl 11-aminoundecanoate
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-129773
-
|
Phthalimide-PEG4-PDM-OTBS
|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG4-PDM-OTBS is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-PDM-OTBS can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-148362
-
-
- HY-150226
-
|
Enzyme-IN-1
|
Proteasome
|
Inflammation/Immunology
|
|
Enzyme-IN-1 (compound 1) is a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases. Specifically, Enzyme-IN-1 inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. Enzyme-IN-1 may has potential antiinflammatory properties.
|
-
- HY-P2972
-
-
- HY-111546
-
|
BI-3663
|
PROTACs
FAK
|
Cancer
|
|
BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.
|
-
- HY-144323
-
|
YF135
|
PROTACs
PERK
|
Cancer
|
|
YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
|
-
- HY-130822
-
|
K-Ras ligand-Linker Conjugate 4
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-130823
-
|
K-Ras ligand-Linker Conjugate 5
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-136055
-
-
- HY-133045
-
|
VHL Ligand 8
|
Ligands for E3 Ligase
|
Cancer
|
|
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-125876
-
|
PROTAC Bcl2 degrader-1
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, 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.
|
-
- HY-131911
-
-
- HY-145071
-
|
PROTAC ERα Y537S degrader-1
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader.
|
-
- HY-130707
-
|
K-Ras ligand-Linker Conjugate 3
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-130652
-
|
Pomalidomide 4'-PEG3-azide
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1 degrader based on Rucaparib by using the PROTAC approach.
|
-
- HY-129772
-
|
Phthalimide-PEG3-C2-OTs
|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-40178
-
|
NH2-C4-NH-Boc
|
PROTAC Linkers
|
Cancer
|
|
NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-110174
-
|
NAB2
|
Others
|
Neurological Disease
|
|
NAB2 is a neuron-protective agent. NAB2 strongly and selectively protects diverse cell types from α-syn toxicity. NAB2 promots endosomal transport events dependent on the E3 ubiquitin ligase Rsp5/Nedd4. NAB2 identifies a agentgable node in the biology of α-syn that can correct multiple aspects of its underlying pathology, including dysfunctional endosomal and endoplasmic reticulum-to-Golgi vesicle trafficking.
|
-
- HY-103636
-
|
PROTAC Sirt2 Degrader-1
|
Sirtuin
PROTACs
|
Cancer
|
|
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
|
-
- HY-130122
-
|
MG-277
|
Molecular Glues
PROTACs
Apoptosis
|
Cancer
|
|
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.
|
-
- HY-151791
-
|
(S,R,S)-AHPC-C6-PEG3-butyl-N3
|
ADC Linker
|
Others
|
|
(S,R,S)-AHPC-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. (S,R,S)-AHPC-C6-PEG3-butyl-N3 serves as crosslinker-E3 ligase ligand conjugate, Click reactive protein degrader building block for PROTAC research, Template for synthesis of targeted protein degrader, VH032 conjugate.
|
-
- HY-131168
-
-
- HY-129619
-
|
SNIPER(ER)-87
|
SNIPERs
Estrogen Receptor/ERR
|
Cancer
|
|
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
|
-
- HY-123941
-
|
FKBP12 PROTAC dTAG-7
dTAG-7
|
PROTACs
FKBP
Epigenetic Reader Domain
|
Cancer
|
|
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
|
-
- HY-146177
-
|
CYP3A4 enzyme-IN-1
|
Bacterial
Cytochrome P450
|
Infection
|
|
CYP3A4 enzyme-IN-1 (compound 59) is a potent antibacterial agent, with a MIC of 1 μg/mL for MRSA. CYP3A4 enzyme-IN-1 exhibits low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6, and CYP3A4 enzymes.
|
-
- HY-W050162
-
|
(E)-3,4,5-Trimethoxycinnamic acid
TMCA
|
GABA Receptor
5-HT Receptor
|
Neurological Disease
|
|
(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.
|
-
- HY-136006
-
-
- HY-133487B
-
-
- HY-137516
-
|
LC-2
|
PROTACs
Ras
|
Cancer
|
|
LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.
|
-
- HY-136006A
-
-
- HY-130422
-
|
Tos-PEG4-t-butyl ester
Tos-PEG4-Boc
|
PROTAC Linkers
|
Cancer
|
|
Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker, which refers to the PEG composition. Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) can be used in the synthesis of a series of PROTACs, such as BI-3663 (HY-111546). BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation, and inhibits PTK2 with an IC50 of 18 nM.
|
-
- HY-130618
-
|
Boc-C1-PEG3-C4-OH
|
PROTAC Linkers
|
Cancer
|
|
Boc-C1-PEG3-C4-OH is a PROTAC linker, which refers to the Alkyl/ether composition. Boc-C1-PEG3-C4-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-133487
-
-
- HY-130711A
-
|
(S,R,S)-AHPC-C3-NH2 TFA
VH032-C3-NH2 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
|
-
- HY-130711
-
|
(S,R,S)-AHPC-C3-NH2
VH032-C3-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
|
-
- HY-P2876
-
-
- HY-124861
-
-
- HY-R03202
-
|
mmu-miR-467e-3p mimic
|
MicroRNA
|
Cancer
|
|
mmu-miR-467e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R00543
-
|
hsa-miR-30e-3p mimic
|
MicroRNA
|
Cancer
|
|
hsa-miR-30e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R03049
-
|
mmu-miR-344e-3p mimic
|
MicroRNA
|
Cancer
|
|
mmu-miR-344e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R01681
-
|
hsa-miR-548e-3p mimic
|
MicroRNA
|
Cancer
|
|
hsa-miR-548e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R01601
-
|
hsa-miR-520e-3p mimic
|
MicroRNA
|
Cancer
|
|
hsa-miR-520e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R01572
-
|
hsa-miR-518e-3p mimic
|
MicroRNA
|
Cancer
|
|
hsa-miR-518e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R03465
-
|
mmu-miR-669e-3p mimic
|
MicroRNA
|
Cancer
|
|
mmu-miR-669e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R00009
-
|
hsa-let-7e-3p mimic
|
MicroRNA
|
Cancer
|
|
hsa-let-7e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R01593
-
|
hsa-miR-519e-3p mimic
|
MicroRNA
|
Cancer
|
|
hsa-miR-519e-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-W068771
-
-
- HY-A0003S
-
|
Lenalidomide-d5
CC-5013-d5
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
|
-
- HY-151792
-
|
Pomalidomid-C6-PEG3-butyl-N3
|
PROTACs
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.
Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader.
|
-
- HY-131387
-
-
- HY-N1414
-
-
- HY-P2807
-
-
- HY-P2935
-
-
- HY-129602
-
|
SD-36
|
PROTACs
STAT
Apoptosis
|
Cancer
|
|
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase.
|
-
- HY-142444
-
|
SSAO/VAP-1 inhibitor 1
|
AP-1
|
Metabolic Disease
|
|
SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3).
|
-
- HY-112495
-
|
VH032-PEG5-C6-Cl
HaloPROTAC 2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. VH032-PEG5-C6-Cl incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-130619
-
|
Boc-C1-PEG3-C4-OBn
|
PROTAC Linkers
|
Cancer
|
|
Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-W012845A
-
-
- HY-129430
-
-
- HY-P2999
-
|
Endo-β-N-acetylglucosaminidase
ENGase
|
Endogenous Metabolite
|
Others
|
|
Endo-β-N-acetylglucosaminidase (ENGase) is cytosolic deglycosylating enzyme that hydrolyzes the N-linked oligosaccharides. Endo-β-N-acetylglucosaminidase can be used for glycan analysis on glycoproteins and preparation of precursors for glycosylated compounds, is often used in biochemical studies.
|
-
- HY-145177
-
|
Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader. (From patent WO2017180417A1 compound s7).
|
-
- HY-P2931
-
|
Triosephosphate isomerase
TPI
|
Endogenous Metabolite
|
Others
|
|
Triosephosphate isomerase (TPI) is a glycolytic enzyme. Triosephosphate isomerase fast interconverts dihydroxyacetone phosphate and D: -glyceraldehyde-3-phosphate, its catalytic site is at the dimer interface.
|
-
- HY-P2921
-
|
Urate oxidase
Uox
|
Endogenous Metabolite
|
Others
|
|
Urate oxidase (Uox), i.e., uricase, is often used in biochemical studies. Urate oxidase is a peroxisomal enzyme that catalyzes the oxidation of uric acid to allantoin in most mammals.
|
-
- HY-131187
-
|
BMS-1166-N-piperidine-COOH
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-138102
-
|
SSAA09E3
|
SARS-CoV
|
Infection
|
|
SSAA09E3 is a SARS-CoV entry inhibitor that inhibits SARS/HIV pseudotyped virus entry with an EC50 of 9.7 μM in 293T cells and inhibits SARS-CoV infection of Vero cells with an EC50 of 0.15 μM.
|
-
- HY-P2818
-
-
- HY-P1635
-
|
Pepsin A
|
Endogenous Metabolite
|
Endocrinology
|
|
Pepsin A is the major pig and human gastric proteases, it is a pepsin-like minor gastric proteolytic enzymes. Pepsin A contributes to proteolysis of food proteins in the vertebrate stomach.
|
-
- HY-P9934
-
|
Abciximab
C7E3
|
Integrin
|
Cardiovascular Disease
|
|
Abciximab (C7E3), a chimeric mouse/human monoclonal antibody, is a glycoprotein (GP) IIb/IIIa inhibitor. Abciximab inhibits platelet aggregation and leucocyte adhesion by binding to the glycoprotein IIb/IIIa, vitronectin and Mac-1 receptors.
|
-
- HY-W068783
-
-
- HY-P2911
-
|
Glutamate dehydrogenase (NAD(P))
GLDH
|
Mitochondrial Metabolism
|
Others
|
|
Glutamate dehydrogenase NAD(P) (GLDH) can be found in hepatocytes, renal tissue, brain, muscle, and intestinal cells. Glutamate dehydrogenase NAD(P) is often used in biochemical studies. Glutamate dehydrogenase is a mitochondrial enzyme, it catalyzes the reversible oxidative deamination of glutamate to α-ketoglutarate (α-KG) as part of the urea cycle.
|
-
- HY-P2994
-
|
3-Hydroxybutyrate dehydrogenase
3-HBDH
|
Endogenous Metabolite
|
Others
|
|
3-Hydroxybutyrate dehydrogenase (3-HBDH) is a mitochondrial enzyme, is often used in biochemical studies. 3-hydroxybutyrate dehydrogenase is involved in the synthesis and degradation of ketone bodies and butanoate metabolism. 3-Hydroxybutyrate dehydrogenase catalyzes (R)-3-hydroxybutanoate converts into acetoacetate.
|
-
- HY-N11650
-
|
(22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid
|
Bacterial
|
Infection
|
|
(22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid (compound 15) is an antitubercular agent with MIC value of 12.5 μg/mL for Mycobacterium tuberculosis H37Ra. (22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid shows cytotoxicity with IC50 value of 32 μM for Vero cells.
|
-
- HY-116750
-
|
6-Hydroxykaempferol
|
Others
|
Others
|
|
6-Hydroxykaempferol, a flavonoid, is a competitive tyrosinase inhibitor with an IC50 value of 124 μM. 6-Hydroxykaempferol has a Ki value of 148 μM relative to L-DOPA as a substrate and effectively inhibits the activity of the enzyme by binding to the active site of the enzyme.
|
-
- HY-E70003
-
-
- HY-131183
-
|
PROTAC PD-1/PD-L1 degrader-1
|
PROTACs
PD-1/PD-L1
|
Inflammation/Immunology
|
|
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
|
-
- HY-130654
-
|
(S,R,S)-AHPC-C2-PEG4-N3
VH032-C2-PEG4-N3
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM.
|
-
- HY-N10383
-
-
- HY-116677
-
-
- HY-108285
-
|
(Rac)-Telmesteine
|
Others
|
Inflammation/Immunology
|
|
(Rac)-Telmesteine is a protease inhibitor and is thus a suitable enzyme stabilizer extracted from patent WO 2017220302 A1, compound II-1. (Rac)-Telmesteine can be used as an enzyme stabilizer in protease-containing detergents and cleaning agents.
|
-
- HY-N1778A
-
-
- HY-P2802
-
|
α-Glucosidase
α-D-Glucosidase
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase (α-D-Glucosidase), a carbohydrate hydrolyzing enzyme, catalyzes the liberation of α-glucose from the non-reducing end of the substrate. α-Glucosidase can facilitate the absorption of glucose by the small intestine. Inhibition of α-Glucosidase is an effective management of non-insulin-dependent diabetes mellitus (NIDDM).
|
-
- HY-W015495
-
-
- HY-10082A
-
|
(E)-3-AP
(E)-PAN-811; (E)-NSC# 663249; (E)-OCX191
|
DNA/RNA Synthesis
|
Cancer
|
|
(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis.
|
-
- HY-125863
-
|
Glucose-6-phosphate dehydrogenase
|
Endogenous Metabolite
|
Cancer
Metabolic Disease
|
|
Glucose-6-phosphate dehydrogenase is the rate-limiting enzyme of the pentose phosphate pathway. Glucose-6-phosphate dehydrogenase is a major source of NADPH that is required by many essential cellular systems including the antioxidant pathways, nitric oxide synthase, NADPH oxidase, cytochrome p450 system, and others. Glucose-6-phosphate dehydrogenase can be used for the research of diabetes, aldosterone-induced endothelial dysfunction, and cancer.
|
-
- HY-134459
-
-
- HY-135849
-
|
Catalase
|
Reactive Oxygen Species
|
Cancer
|
|
Catalase is a key enzyme in the metabolism of H2O2 and reactive oxygen species (ROS), and its expression and localization is markedly altered in tumors. Free oxygen radical scavenger.
|
-
- HY-139162
-
|
BGN3
|
Others
|
Others
|
|
BGN3 is a good substrate for the SNAP-tag ® and H 5 enzymes. The activities of SNAP-tag ® and H 5 enzymes on BGN3 are reasonable (IC50= 15.6 and 23.5 μM, respectively).
|
-
- HY-139163
-
|
BGSN3
|
Others
|
Others
|
|
BGSN3 is a good substrate for the SNAP-tag ® and H 5 enzymes. The activities of SNAP-tag ® and H 5 enzymes on BGSN3 are reasonable (IC50=17.8 and 10 μM, respectively).
|
-
- HY-111997
-
|
VH285-PEG4-C4-Cl
HaloPROTAC 3
|
E3 Ligase Ligand-Linker Conjugates
|
|
|
VH285-PEG4-C4-Cl (HaloPROTAC 3) is a conjugate of ligands for E3 and 16-atom-length linker. The connector of linker is Halogen group. VH285-PEG4-C4-Cl incorporates the VH285 based VHL ligand and an alkyl/ether-based linker. VH285-PEG4-C4-Cl is a highly potent and efficacious degrader of GFP-HaloTag7 with a DC50 of 19 nM. VH285-PEG4-C4-Cl is able to induce 90 % degradation of GFP-Halotag at 625 nM. VH285-PEG4-C4-Cl binds to VHL with an IC50 of 0.54 μM.
|
-
- HY-N10191
-
-
- HY-B2192
-
|
Amylase
|
Others
|
Metabolic Disease
|
|
Amylase is an enzyme produced by pancreas and salivary glands, catalyzing the hydrolysis of starch into sugars. Amylase are broadly classified into α, β, and γ subtypes.
|
-
- HY-P3948
-
-
- HY-121517
-
|
URB754
|
Others
|
Neurological Disease
|
|
URB754 is a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) with an IC50 of 200 nM.
|
-
- HY-P3991
-
-
- HY-133927
-
-
- HY-W411361
-
-
- HY-126399
-
|
Bis-tris propane
BTP
|
Biochemical Assay Reagents
|
Others
|
|
Bis-tris propane (BTP) is a water-soluble buffer substance. Bis-tris propane can be used as a suitable buffer for polymerase chain reaction (PCR). Bis-tris propane can enhance the stability or activity of restriction enzymes.
|
-
- HY-146125
-
|
CGCG/CGG ligand 1
|
Others
|
Metabolic Disease
|
|
CGCG/CGG ligand 1 (compound 10), an anthracenone derivative, is a CGCG or CGG short spacer-ligand. CGCG/CGG ligand 1 can protect cleavable sites of DNA with the multiple CGCG or continuous CGG sites from the restriction enzyme.
|
-
- HY-B0382
-
-
- HY-107393
-
-
- HY-P3947
-
-
- HY-150621
-
|
AS1134900
|
Others
|
Cancer
|
|
AS1134900 is a highly selective, allosteric and uncompetitive NADP +-dependent malic enzyme 1 (ME1) inhibitor.
|
-
- HY-B1746
-
-
- HY-P3141
-
-
- HY-125965
-
|
BioA-IN-13
|
Bacterial
|
Infection
|
|
BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.
|
-
- HY-33914
-
-
- HY-117878
-
|
ML345
|
Others
|
Metabolic Disease
|
|
ML345 is a potent and selective insulin-degrading enzyme (IDE) small-molecule inhibitor, with an IC50 value of 188 nM. ML345 can be for use as a pharmacophore for agent development in diabetes research.
|
-
- HY-W090942
-
-
- HY-D1534
-
-
- HY-148190
-
|
Sheng Gelieting
CGT-8012
|
Dipeptidyl Peptidase
|
Endocrinology
|
|
Sheng Gelieting (CGT-8012) is a dipeptidy peptidase-IV enzyme (DP-IV) inhibitor. Sheng Gelieting has great DP-IV inhibition activity with an IC50 value of 87 nM. Sheng Gelieting can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete.
|
-
- HY-143401
-
|
Hit 1
|
Others
|
Metabolic Disease
|
|
Hit 1 is an activator of ansulin degrading enzyme (IDE), with an EC50 of 5.5 μM. Hit 1 can decrease glucose-stimulating insulin secretion.
|
-
- HY-B0690
-
-
- HY-P4560
-
|
H-Pro-Phe-OH
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
H-Pro-Phe-OH is a dipeptide containing proline and phenylalanine, which can serve as a substrate for prolinase. H-Pro-Phe-OH can also be used for polypeptide synthesis, where phenylalanine is an aromatic amino acid that can inhibit the activity of Angiotensin-converting enzyme (ACE, HY-P2983).
|
-
- HY-B1433
-
-
- HY-152252
-
|
Antibacterial agent 133
|
Bacterial
Fungal
|
Infection
|
|
Antibacterial agent 133 (4l) is an antimicrobial agent that has shown anti-Candida activity, particularly through LMD enzyme inhibition. Antibacterial agent 133 shows MIC90 values of 1.95 μg/mL against Candida albicans ATCC 24433, Candida smoothis ATCC 90030 and Candida subtilis ATCC 22019.
|
-
- HY-137875
-
-
- HY-135470
-
|
Nifurpirinol
P-7138
|
Antibiotic
Bacterial
|
Infection
|
|
Nifurpirinol (P-7138) is a nitroaromatic antibiotic and acts as a novel substrate for the bacterial nitroreductase (NTR) enzyme. Nifurpirinol is a more potent proagent compared to Metronidazole to trigger cell-ablation in nitroreductase expressing transgenic models.
|
-
- HY-N2021
-
-
- HY-145954
-
|
NAT2-IN-1
APA
|
Others
|
Cancer
|
|
NAT2-IN-1 (APA) is an inhibitor of agent metabolic enzyme N-acetyltransferase 2 (NAT2). NAT2-IN-1 can selectively kill slow NAT2 cells.
|
-
- HY-N2021A
-
-
- HY-114879
-
|
DDAO
|
Fluorescent Dye
|
Cancer
|
|
DDAO is a promising near-infrared (NIR) red fluorescent probe?with tunable excitation wavelength (600-650?nm) and long?emission wavelength?(λem?=?656?nm). DDAO can de desiged for detection of the activities of different enzymes such as?β-galactosidase,?sulfatase, protein?phosphatase?2A,?carboxylesterase 2, human?albumin and?esterases. Storage: protect from light.
|
-
- HY-E70078
-
-
- HY-121460
-
-
- HY-P3749
-
|
Mca-(ala7,lys(dnp)9)-bradykinin
|
Fluorescent Dye
|
Others
|
|
Mca-(ala7,lys(dnp)9)-bradykinin is a sensitive fluorogenic substrate for ECE-1 (endothelin-converting enzyme-1). The incorporation of a (7-methoxycoumarin-4-yl)acetyl (Mca) fluorescent group and a 2,4-dinitrophenyl (Dnp) quenching group has resulted in a large fluorescence increase upon substrate cleavage.
|
-
- HY-150548
-
|
COX-2/15-LOX-IN-1
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
COX-2/15-LOX-IN-1 (Compound 14) is a COX-2 and 15-lipoxygenase enzyme (15-LOX) inhibitor with IC50 values of 10.65, 0.075 and 2.98 μM against COX-1, COX-2 and 15-LOX, respectively. COX-2/15-LOX-IN-1 shows anti-inflammatory activity.
|
-
- HY-33298
-
|
LM10
|
Others
|
Cancer
|
|
LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO). Tryptophan 2,3-dioxygenase (TDO) is an unrelated hepatic enzyme that also degrades tryptophan along the kynurenine pathway. LM10 has the potential for the research of cancer diseases.
|
-
- HY-118660
-
|
Anhydrotetracycline hydrochloride
|
Antibiotic
Bacterial
|
Infection
|
|
Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells.
|
-
- HY-N7335
-
-
- HY-138843
-
-
- HY-78961
-
-
- HY-111558
-
|
Bobcat339
|
DNA Methyltransferase
TET Protein
|
Cancer
|
|
Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
|
-
- HY-138843A
-
-
- HY-143432
-
|
Cdc7-IN-18
|
CDK
|
Cancer
|
|
Cdc7-IN-18 (compound 1-2) is a potent CDC7 inhibitor with an IC50 of 1.29 nM for Cdc7/DBF4 enzyme. Cdc7-IN-18 shows antiproliferative activities with IC50 of 53.62 nM in COLO205 cells.
|
-
- HY-P2778
-
-
- HY-A0116A
-
-
- HY-A0116
-
-
- HY-P2806
-
-
- HY-W030319
-
-
- HY-135024
-
|
Phenylacetyl CoA
Phenylacetyl Coenzyme A
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phenylacetyl CoA is an acceptor oxidoreductase. Phenylacetyl CoA is a membrane-bound molybdenum–iron–sulfur enzyme involved in anaerobic metabolism of phenylalanine in the denitrifying bacterium Thauera aromatica.
|
-
- HY-147388
-
|
hiCE inhibitor-1
|
Others
|
Metabolic Disease
|
|
hiCE inhibitor-1, a sulfonamide derivative, is a selective human intestinal enzyme (hiCE) inhibitor with a Ki value of 53.3 nM. hiCE inhibitor-1 can be used to improve Irinotecan (HY-16562)-induced diarrhoea.
|
-
- HY-P3190
-
-
- HY-P2756
-
-
- HY-114175
-
-
- HY-P2998
-
-
- HY-108647
-
|
EO 1428
|
p38 MAPK
|
Inflammation/Immunology
|
|
EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation.
|
-
- HY-115537
-
|
NAE-IN-M22
|
Apoptosis
|
Cancer
|
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
|
-
- HY-E70077
-
|
Penicillinase (from calf stomach)
|
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
Penicillinase (from calf stomach) is an enzyme that degrades penicillin by hydrolyzing the cyclic amide bonds in the lactam ring of penicillin, which can inactivate penicillin. Penicillinase (from calf stomach) can be isolated from penicillin resistant strains. Penicillinase (from calf stomach) has potential application as a marker for steroid hormone enzyme linked immunosorbent assay.
|
-
- HY-122886
-
|
XL 188
|
Deubiquitinase
|
Cancer
|
|
XL 188 is a potent and selective USP7 inhibitor with IC50 values of 90 nM and 193 nM for USP7 full-length and catalytic domain enzyme, respectively. XL 188 can be used in research of cancer.
|
-
- HY-130569
-
|
7-Hydroxymethotrexate
|
Drug Metabolite
|
Cancer
Inflammation/Immunology
|
|
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
-
- HY-152250
-
|
Antibacterial agent 132
|
Cytochrome P450
Bacterial
|
Infection
|
|
Antibacterial agent 132 has anticandidal effects against C. parapsilosis (ATCC 22019) and C. krusei (ATCC 6258) with MIC90 values of <0.06 μg/mL and 62.50 μg/mL, respectively. Antibacterial agent 132 inhibits aromatase enzyme with an IC50 of 0.047μM.
|
-
- HY-120019A
-
|
Ac-YVAD-CHO acetate
L-709049 acetate
|
Interleukin Related
Caspase
Apoptosis
|
Inflammation/Immunology
|
|
Ac-YVAD-CHO (L-709049) acetate is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO acetate is also a caspase-1 inhibitor. Ac-YVAD-CHO acetate can suppress the production of mature IL-lβ.
|
-
- HY-120019
-
|
Ac-YVAD-CHO
L-709049
|
Interleukin Related
Apoptosis
Caspase
|
Inflammation/Immunology
|
|
Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO is also a caspase-1 inhibitor. Ac-YVAD-CHO can suppress the production of mature IL-lβ.
|
-
- HY-151806
-
|
HadAB-IN-1
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
HadAB-IN-1 is a potent HadAB inhibitor. HadAB-IN-1 inhibits HadAB enzyme complexes activity with an IC50 value of 0.03 μM. HadAB-IN-1 also affects mycolic acid biosynthesis in Mycobacterium tuberculosis (Mtb). HadAB-IN-1 can be used for the research of tuberculosis (TB).
|
-
- HY-146379
-
|
SARS-CoV-2-IN-19
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-19 (Compound 6g) is a potent inhibitor of SARS-CoV-2 with an EC50 of 8.8 μM. SARS-CoV-2-IN-19 shows potent activity against SARS-CoV-2 helicase (nsp13), a highly conserved enzyme, highlighting a potentiality against emerging HCoVs outbreaks. SARS-CoV-2-IN-19 has the potential for the research of infection diseases.
|
-
- HY-P2979
-
|
Invertase
|
Endogenous Metabolite
|
Others
|
|
Invertase is a major enzyme present in plants and microorganisms, is often used in biochemical studies. Invertase catalyzes the hydrolysis of the disaccharide sucrose into glucose and fructose.
|
-
- HY-P2726
-
-
- HY-B2237A
-
|
Lysozyme chloride
|
Bacterial
HIV
|
Infection
|
|
Lysozyme chloride is a bactericidal enzyme, and it lyses gram-positive bacteria. Lysozyme chloride can also be used for the research of HIV infection and pulmonary emphysema.
|
-
- HY-110197
-
|
6bK TFA
|
Others
|
Metabolic Disease
|
|
6bK TFA is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK TFA increases circulating insulin in high-fat-fed mice. Acute administration of 6bK TFA enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice.
|
-
- HY-125798
-
|
2,3-Dehydro-2-deoxy-N-acetylneuraminic acid
Neu5Ac2en; DANA
|
Influenza Virus
|
Infection
|
|
N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid (Neu5Ac2en) is a potent neuraminidase (sialidase) inhibitor. N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid shows inhibitory activities against human neuraminidase enzymes with IC50s of 143, 43, 61, and 74 μM for NEU1, NEU2, NEU3, and NEU4, respectively. Anti-influenza virus activity.
|
-
- HY-125860
-
|
Tyrosinase
Polyphenol oxidase
|
Tyrosinase
|
Metabolic Disease
|
|
Tyrosinase (Polyphenol oxidase) is a rate-limiting enzyme that controls the production of melanin and is encoded by TYR gene. Tyrosinase is mainly found in melanosomes synthesized by skin melanocytes.
|
-
- HY-P1748
-
|
Thermolysin
TML
|
Endogenous Metabolite
|
Infection
|
|
Thermolysin is a thermostable neutral metalloproteinase enzyme secreted by the Gram-positive bacteria Bacillus thermoproteolyticus. Thermolysin catalyzes the hydrolysis of peptide bonds containing hydrophobic residues.
|
-
- HY-P2820
-
|
Phosphoglucomutase
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phosphoglucomutase is often used in biochemical studies. Phosphoglucomutase is an enzyme that can transfer the phosphate group on the α-D-glucose monomer forward from the 1-position to the 6-position or reversely transfer from the 6-position to the 1-position, and promote the glucose-1-phosphate and glucose-6-phosphate Transform each other. Phosphoglucomutase is a key enzyme in glycolysis and gluconeogenesis, and plays an important role in the metabolism of proteins, lipids and nucleic acids.
|
-
- HY-P2902
-
|
Glucose oxidase
|
Endogenous Metabolite
|
Cancer
|
|
Glucose oxidase is used in the food and beverage industry as a preservative and stabilizer and is commonly derived from the fungus Aspergillus niger. Glucose oxidase can react with intracellular glucose and oxygen (O2) to produce hydrogen peroxide (H2O2) and gluconic acid, which can cut off the nutrition source of cancer cells and consequently inhibit their proliferation.
|
-
- HY-E70079
-
-
- HY-P2877
-
|
Tannase
|
Endogenous Metabolite
|
Others
|
|
Tannase, also known as tanninyl hydrolase, is an enzyme that can hydrolyze ester bonds and tannic acid side bonds, releasing glucose and gallic acid, and is outstanding in clarifying wine and fruit juice.
|
-
- HY-P2755
-
-
- HY-W040256
-
-
- HY-P2895
-
|
Clostripain
Clostridiopeptidase B
|
Endogenous Metabolite
|
Others
|
|
Clostripain (Clostridiopeptidase B) is a proteolytic enzyme isolated from Clostridium histolyticum with esterase, amidase and protease activities and is a highly specific carboxypeptide targeting arginine key protease.
|
-
- HY-P2986
-
-
- HY-P2740
-
|
Alcohol dehydrogenase
EC 1.1.1.1
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Alcohol dehydrogenase is a dimeric protein in the cytosol of cells. Alcohol dehydrogenase, the key enzyme for alcohol consumption in the body, is the highest expressed in the liver and participates in the detoxification mechanism of environmental alcohol.
|
-
- HY-P2887
-
|
Acetate kinase (ACK)
|
Endogenous Metabolite
|
Others
|
|
Acetate kinase (ACK) is an enzyme widely distributed in bacteria and archaea. In the presence of ATP and divalent cations, it catalyzes the phosphorylation of acetate and promotes the production of acetyl-CoA. Often used in biochemical research.
|
-
- HY-144169
-
-
- HY-144371
-
-
- HY-E70005
-
|
Collagenase
|
Biochemical Assay Reagents
|
Others
|
|
Collagenase is a proteolytic enzyme, which breaks the peptide bonds in collagen. Collagenase has good research potential in disc herniation, keloid, cellulite, lipoma, as well as peyronie's disease and dupuytren fracture.
|
-
- HY-P2742
-
|
Ascorbate oxidase
ASO
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Ascorbate oxidase, also known as vitamin C oxidase, is a REDOX enzyme involved in the regulation of extracellular matrix. Ascorbate oxidase catalyzes the reaction of ascorbic acid and oxygen to produce dehydroascorbic acid.
|
-
- HY-P2943
-
|
Phosphate acetyltransferase
|
Endogenous Metabolite
|
Others
|
|
Phosphate acetyltransferase is a transferase enzyme, is often used in biochemical studies. Phosphate acetyltransferase catalyzes the reversible transfer of the acetyl group from acetyl-P to CoA forming acetyl-CoA and inorganic phosphate, participating to acetate assimilation/dissimilation reactions.
|
-
- HY-P2891
-
|
Pyruvate oxidase
PoxB
|
Endogenous Metabolite
|
Others
|
|
Pyruvate oxidase (PoxB) is a thiamine pyrophosphate-dependent oxidase that catalyzes the oxidative decarboxylation of pyruvate to acetyl phosphate, carbon dioxide and water. Pyruvate oxidase is an important enzyme in bacterial metabolism and is often used in biochemical research.
|
-
- HY-P2799
-
-
- HY-E70012
-
-
- HY-P3016
-
|
Aspartate aminotransferase
AST
|
Endogenous Metabolite
|
Others
|
|
Aspartate aminotransferase (AST) is a transaminase enzyme, is often used in biochemical studies. Aspartate aminotransferase catalyzes aspartate and alpha-ketoglutarate converts to oxaloacetate and glutamate. Aspartate aminotransferase can be found in cerebrospinal fluid, exudates, and transudates.
|
-
- HY-P2776
-
|
Hexokinase (ScHEX1)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hexokinase (ScHEX1) is a glycolytic enzyme hexokinase that is inhibited by n-acetylglucosamine. Inhibition of Hexokinase (ScHEX1) by n-acetylglucosamine leads to its separation from the mitochondrial outer membrane, resulting in activation of NLRP3 inflammasome.
|
-
- HY-E70014
-
|
Glucose 1-dehydrogenase
FAD-GDH
|
Endogenous Metabolite
|
Others
|
|
Glucose 1-dehydrogenase, or glucose dehydrogenase (FAD)/Pseudomonas glucose dehydrogenase. Glucose 1-dehydrogenase is an enzyme used as a regeneration cofactor to convert glucose and NAD(P) into NAD(P)H and gluconic acid.
|
-
- HY-149048
-
|
Adenosylhomocysteinase
SAHH; AHCY
|
Endogenous Metabolite
HBV
|
Infection
Metabolic Disease
|
|
Adenosylhomocysteinase (SAHH; AHCY) is a highly conserved enzyme. Adenosylhomocysteinase reversible catalyzes S-adenosylhomocysteine (SAH) to adenosine and L-homocysteine. The serum exosomal Adenosylhomocysteinase level can be used as a prognostic biomarker in HBV-LC patients.
|
-
- HY-E70076
-
|
Subtilisin (Compound proteinase)
|
Biochemical Assay Reagents
|
Others
|
|
Subtilisin (Compound proteinase) is a proteolytic enzyme. Subtilisin (Compound proteinase) has catalytic activity in anhydrous dimethyl formamide. Subtilisin (Compound proteinase) can be used as a catalyst for easy coupling between sugars and amino acids.
|
-
- HY-P2952
-
|
Adenylate
AMPK; Myokinase; Adk
|
Endogenous Metabolite
|
Others
|
|
Adenylate (Adk), i.e., myokinase, is a phosphotransferase enzyme, is often used in biochemical studies. Adenylate catalyzes the interconversion of adenosine phosphates. Adenylate monitors phosphate nucleotide levels inside the cell, it plays an important role in cellular energy homeostasis.
|
-
- HY-W353804
-
|
2′-Deoxy-β-L-uridine
|
Nucleoside Antimetabolite/Analog
|
Infection
|
|
2'-Deoxy-β-L-uridine is a nucledside analogue and a specific substrate for the viral enzyme, shows no stereospecificity against herpes simplex 1 (HSV1) thymidine kinase (TK). 2′-Deoxy-β-L-uridine exerts antiviral activity via the interation of 5'-triphosphates with the viral DNA polymerase.
|
-
- HY-143285
-
|
AMC-GlcNAc
|
Fluorescent Dye
|
|
|
AMC-GlcNAc (compound 1) is a potent fluorogenic probe for detection and characterization of β-hexosaminidase enzyme activity. AMC-GlcNAc enables continuous monitoring by turn-on fluorescence and fluorescence signal is constant over a wide pH range (Ex=325 nm, Em=390 nm). AMC-GlcNAc enables ratiometric fluorescence detection with high sensitivity and low background, which can be used to screen for recombinant dispersin B activity in E. coli cell lysate. Storage: protect from light.
|
-
- HY-125604
-
|
WCK-4234
|
Bacterial
|
Infection
|
|
WCK-4234 is a potent β-lactamase inhibitor. WCK-4234 inhibits class A, C, and D β-lactamases activity. WCK-4234 lacks direct antibacterial activity. WCK-4234 potentiates imipenem and meropenem against Enterobacteriaceae with OXA-48/OXA-181 or KPC enzymes, or with combinations of impermeability and AmpC or ESBL activity. WCK-4234 distinctively overcomes resistance mediated by OXA-type carbapenemases.
|
-
- HY-P1923
-
|
L-Asparaginase
L-ASNase
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis.
|
-
- HY-19676
-
|
Pralnacasan
VX-740; HMR 3480
|
Caspase
|
Inflammation/Immunology
|
|
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.
|
-
- HY-E70010
-
|
Aldose 1-epimerase
mutarotases
|
Endogenous Metabolite
|
Others
|
|
Aldose 1-epimerase (mutarotases) is a key enzyme of carbohydrate metabolism catalysing the interconversion of the α- and β-anomers of hexose sugars such as glucose and galactose. Aldose 1-epimerase is essential for normal carbohydrate metabolism and the production of complex oligosaccharides.
|
-
- HY-P3029
-
|
Phospholipase A2
PLA2
|
Phospholipase
|
Others
|
|
Phospholipase A2 (PLA2) catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid (AA). Phospholipase A2 is a member of the class of heat-stable, calcium-dependent enzymes, is often used in biochemical studies.
|
-
- HY-P2875
-
|
Hemicellulase
|
Endogenous Metabolite
|
Others
|
|
Hemicellulase belongs to the enzyme family of glycoside hydrolase, which is often used in biochemical research. Hemicellulase can disrupt the binding of glucose and polymers present in plant fibers to water molecules, and is a key component in the degradation of plant biomass and carbon flow in nature.
|
-
- HY-P2993
-
|
Isocitrate dehydrogenase
ICDH
|
Isocitrate Dehydrogenase (IDH)
|
Metabolic Disease
|
|
Isocitrate dehydrogenase (ICDH) is a citric acid or tricarboxylic acid cycle enzyme, is often used in biochemical studies. Isocitrate dehydrogenase catalyzes the oxidative decarboxylation of isocitrate to α-ketoglutarate and reduces NAD(P) + to NAD(P)H, it plays important roles in cellular metabolism.
|
-
- HY-E70037
-
|
GlcNAc kinase (EcNagK)
N-Acetylglucosamine kinase
|
Endogenous Metabolite
|
Metabolic Disease
|
|
GlcNAc kinase (EcNagK) (N-Acetylglucosamine kinase) is a GlcNAc-metabolizing enzyme. GlcNAc kinase (EcNagK) transfers the gamma-phosphoryl group of an ATP onto the hydroxyl group at the C-6 of GlcNAc to generate a GlcNAc-6-P.
|
-
- HY-P2980
-
|
Carboxypeptidase A
EC 3.4.2.1
|
Endogenous Metabolite
|
Others
|
|
Carboxypeptidase A (EC 3.4.2.1) is a zinc-containing metalloprotease, is often used in biochemical studies. Carboxypeptidase A catalyzes the hydrolysis of the peptide bonds that are adjacent to the C-terminal end of a polypeptide chain. Carboxypeptidase A is a prototypical enzyme for metalloproteases that plays important roles in biological systems.
|
-
- HY-153102
-
|
G3-CNP
|
Biochemical Assay Reagents
|
Others
|
|
G3-CNP is an α-amylase substrate. The absorbance of G3-CNP cleavage product 2-chloro-4-nitrophenol is measured at 405 nm, which can be used to detect enzyme activity.
|
-
- HY-D0714
-
|
Tetrazolium Red
2,3,5-Triphenyltetrazolium chloride; TPTZ; TTC
|
Biochemical Assay Reagents
|
Others
|
|
Tetrazolium Red(2,3,5-Triphenyltetrazolium chloride; TPTZ) is used to visualize dehydrogenase enzyme activity; initially the tetrazolium solution is colorless but changes to red when it comes into contact with hydrogen.
|
-
- HY-P2879
-
|
Cholesterol esterase
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Cholesterol esterase is an enzyme that hydrolyzes cholesterol ester to cholesterol and free fatty acid in the intestinal lumen. Cholesterol synthesized in the acinar cells and is stored in zymogen granules. Cholesterol esterase is also known as bile salt-stimulated lipase and carboxy ester lipasea, acts function for acceleration of cholesterol absorption.
|
-
- HY-P2907
-
|
Formate dehydrogenase
|
Endogenous Metabolite
|
Others
|
|
Formate dehydrogenase is an enzyme ubiquitous in prokaryotes and eukaryotes that catalyzes the reversible oxidation of formate to carbon dioxide. According to its metal content, structure and catalytic strategy, Formate dehydrogenase can be divided into two categories, non-metallic and metal-containing, which are often used in biochemical research.
|
-
- HY-P2752
-
|
Lipoprotein lipase
LPL
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lipoprotein lipase Lipoprotein lipase is a multifunctional enzyme from adipose tissue, heart and skeletal muscle, islets and macrophages. Lipoprotein lipase promotes normal lipoprotein metabolism, delivery and utilization of tissue-specific substrates. Lipoprotein lipase catalyzes the rate-limiting step of lipids in blood circulation.
|
-
- HY-P2947
-
|
Aldehyde dehydrogenase (NAD(P))
ALDH
|
Aldehyde Dehydrogenase (ALDH)
|
Others
|
|
Aldehyde dehydrogenase NAD(P) (ALDH) catalyzes the oxidation of aldehydes into their corresponding carboxylic acids with the concomitant reduction of the cofactor NAD(P) into NAD(P)H, is often used in biochemical studies. The aldehyde dehydrogenases (ALDHs) are one of many enzyme systems the body utilizes to alleviate aldehyde stress.
|
-
- HY-E70074
-
|
Monoamine oxidase
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine oxidase is an enzyme composed of different polypeptides. Monoamine oxidation catalyzes the oxidative deamination of various biological amines in brain and peripheral tissues by producing hydrogen peroxide. Monoamine oxidase plays an important role in maintaining the regulation of synaptic transmission, emotional behavior and other brain functions.
|
-
- HY-P2838
-
|
Creatininase
Creatinine amidohydrolase; CAH
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Creatininase (Creatinine amidohydrolase; CAH), namely creatinine amidohydrolase, from Pseudomonas putida, is a homohexameric enzyme commonly used in biochemical research. Creatininase acts on carbon-nitrogen bonds other than peptide bonds, and can catalyze the hydrolysis of creatinine to creatine, which can then be metabolized by creatinase to urea and sarcosine.
|
-
- HY-P3028
-
|
Ficain
Ficin
|
Biochemical Assay Reagents
|
Metabolic Disease
Others
|
|
Ficain is an enzyme extract composed of several proteases that can be isolated from Ficus hispida L. and the latex of fig (Ficus carica). Ficain has different specificities in different proportions during fruit ripening. Ficain is widely used in protein hydrolysis, food, production of bioactive peptides and antibody fragments.
|
-
- HY-147313
-
|
TH10785
|
Others
|
Cancer
Metabolic Disease
|
|
TH10785 is a DNA glycosylase 1 (OGG1) activator, TH10785 can interact with the phenylalanine-319 and glycine-42 amino acids of OGG1 and increase the enzyme activity, generates β, δ-lyase enzymatic function. TH10785 can control the catalytic activity mediated by a nitrogen base within its molecular structure. TH10785 can be used for the research of various diseases and aging connected with DNA oxidative lesions.
|
-
- HY-P2834
-
|
Penicillin amidase
Penicillin acylase
|
Biochemical Assay Reagents
|
Infection
|
|
Penicillin amidase (Penicillin acylase) is an enzyme that cleaves the acyl side chains of penicillins. Penicillin amidase can be used for the production of 6-aminopenicillanic acid. Penicillin amidase can also be used in the resolution of racemic mixtures, peptide synthesis, and synthesis of semi-synthetic β-lactam antibiotics.
|
-
- HY-P2918
-
|
Glucose 6-phosphate isomerase
GPI; Phosphoglucose Isomerase
|
Endogenous Metabolite
|
Others
|
|
Glucose 6-phosphate isomeras (GPI), i.e., phosphoglucose isomerase/phosphoglucoisomerase (PGI) or phosphohexose isomerase (PHI), is often used in biochemical studies. Glucose 6-phosphate isomeras is a highly conserved glycolytic and dimeric enzyme. Glucose 6-phosphate isomeras catalyzes the reversible isomerization of glucose-6-phosphate to fructose-6-phosphate.
|
-
- HY-P3017
-
|
Endo-1,4-β-xylanase
Xylanase; CtXyn11A; EC 3.2.1.8
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Others
|
|
Endo-1,4-β-xylanase (Xylanase) is an arabinoxylan (AX) degrading enzyme and a glycoside hydrolase, is often used in biochemical studies. Endo-1,4-β-xylanase cleaves the β-xylosidic bond between two d-xylopyranosyl residues linked in β-(1,4).
|
-
- HY-E70028
-
|
UDP-sugar pyrophosphorylase (BlUSP)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
UDP-sugar pyrophosphorylase (BlUSP) is the enzyme capable of activating glucose-1-phosphate (Glc-1-P) to UDP-glucose (UDP-Glc). UDP-sugar pyrophosphorylase (BlUSP) catalyzes a reversible transfer of the uridyl group from UTP to sugar-1-phosphate, producing UDP-sugar and pyrophosphate (PPi).
|
-
- HY-131131
-
|
5-CFDA-AM
|
Fluorescent Dye
|
Others
|
|
5-CFDA-AM is a cell-permeable esterase substrate that can be used as an active probe to measure enzyme activity and cell membrane integrity. 5-CFDA-AM is electroneutral and can enter the cell at a lower concentration than CFDA, where it is hydrolysed by intracellular esterases to produce carboxyfluorescein. Carboxyfluorescein contains an additional negative charge and can be better retained in the cell. Storage: protect from light.
|
-
- HY-W067056
-
|
Methyl (E)-cinnamate
Methyl (E)-3-phenylpropenoate
|
Others
|
Inflammation/Immunology
|
|
Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry.
|
-
- HY-P2724
-
|
Purine nucleoside phosphorylase
PNP
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Purine nucleoside phosphorylase is a key enzyme in purine metabolism, which is involved in the purine rescue pathway. The deficiency of Purine nucleoside phosphorylase resulted in impaired T cell function. In the presence of inorganic orthophosphate as the second substrate, Purine nucleoside phosphorylase catalyzes the breaking of the glycosidic bond between ribose and deoxyribonucleoside to generate purine base and ribose (deoxyribose) -1-phosphate.
|
-
- HY-108263B
-
|
(R)-3-Hydroxy Midostaurin
(R)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
|
(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML).
|
-
- HY-142670
-
|
Lp-PLA2-IN-5
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
Lp-PLA2-IN-5 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-5 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 32).
|
-
- HY-142669
-
|
Lp-PLA2-IN-4
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
Lp-PLA2-IN-4 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-4 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 38).
|
-
- HY-P2810
-
|
Rennin
|
Endogenous Metabolite
Ser/Thr Protease
|
Metabolic Disease
|
|
Rennin, also known as Chymosin, is a pepsin-related proteolytic enzyme synthesized by cells in the stomach of certain animals that efficiently converts liquid milk into a semi-solid, allowing it to remain in the stomach for longer. The natural substrate of Rennin is K-casein, which is specifically cleaved at the peptide bond between amino acid residues 105 and 106, phenylalanine and methionine, and is widely used in cheese production.
|
-
- HY-142779
-
|
Lp-PLA2-IN-11
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145).
|
-
- HY-P2812
-
|
Phospholipase D
PLD
|
Phospholipase
|
Cancer
Endocrinology
Inflammation/Immunology
Neurological Disease
|
|
Phospholipase D (PLD) is an enzyme of the phospholipase superfamily, which widely exists in bacteria, yeast, plants, animals and viruses, and is often used in biochemical research. Phospholipase D can catalyze the hydrolysis of phosphodiester bonds in glycerophospholipids to produce phosphatidic acid and soluble choline. Phospholipase D is involved in a variety of disease-related processes, including diabetes, atherogenesis, obesity, tumorigenesis, immune response, and neuroendocrine function.
|
-
- HY-P2860
-
|
Acetylcholinesterase
ACHE; EC 3.1.1.7
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Acetylcholinesterase (ACHE; EC 3.1.1.7) is a cholinergic enzyme mainly found in neuromuscular junctions and cholinergic type chemical synapses, and is often used in biochemical research. Acetylcholinesterase catalyzes the breakdown or hydrolysis of acetylcholine and some other choline esters that act as neurotransmitters into acetate and choline. Acetylcholinesterase's main role is to terminate neuronal transmission and signaling between synapses to prevent ACh spread and activation of nearby receptors.
|
-
- HY-146410
-
|
AT2R antagonist 1
|
Angiotensin Receptor
|
Others
|
|
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes.
|
-
- HY-W015239
-
|
KAT8-IN-1
|
Others
|
Cancer
Inflammation/Immunology
|
|
KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC50s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases.
|
-
- HY-E70050
-
|
beta-1,3-Galactosyltransferase (CgtB)
GM1-synthase
|
Endogenous Metabolite
|
Others
|
|
beta-1,3-Galactosyltransferase (CgtB) (GM1-synthase) is an enzyme that required for sialylated lipooligosaccharide (LOS SIAL) production, is often used in biochemical studies. beta-1,3-Galactosyltransferase (CgtB) catalyzes the addition of a galactose molecule, which is required for GM1-like LOS SIAL structure production.
|
-
- HY-142778
-
|
Lp-PLA2-IN-10
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
Lp-PLA2-IN-10 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-10 has the potential for the research of neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis (extracted from patent WO2022001881A1, compound 4).
|
-
- HY-146000
-
|
Influenza virus-IN-3
|
Influenza Virus
|
Inflammation/Immunology
|
|
Influenza virus-IN-3 (compound 9) is a potent and selective influenza virus inhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM.
|
-
- HY-P2878
-
|
Phosphodiesterase
PDE
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Phosphodiesterase (PDE) is an enzyme that can catalyze the hydrolysis of the 3' ring phosphate bond of cyclic nucleotides, and is often used in biochemical research. Phosphodiesterase acts as an important regulator of signal transduction mediated by the second messenger molecules cAMP and cGMP. According to their specificity to cyclic nucleotides, they can also be divided into different types, such as PDE1-PDE11, which also have certain potential in various diseases.
|
-
- HY-103112A
-
|
SB 243213 dihydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
|
-
- HY-103112B
-
|
SB 243213
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
|
-
- HY-103112
-
|
SB 243213 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
|
-
- HY-N0214A
-
-
- HY-N0214
-
-
- HY-P3878
-
-
- HY-108263A
-
|
(S)-3-Hydroxy Midostaurin
(S)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
|
(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML).
|
-
- HY-P2901
-
|
3α-Hydroxysteroid dehydrogenase
3α-HSD
|
Endogenous Metabolite
|
Endocrinology
|
|
3α-Hydroxysteroid dehydrogenase (3α-HSD) is an enzyme encoded by the AKR1C4 gene, which can catalyze the conversion of 3-ketosteroids into 3α-hydroxy compounds. 3α-Hydroxysteroid dehydrogenase plays an important role in the inactivation of androgen DHT, and can convert DHT into 3α-androstanediol with weak androgen activity, which can be used in the research of hirsutism.
|
-
- HY-129047A
-
|
Trypsin (MS grade)
|
Ser/Thr Protease
Protease Activated Receptor (PAR)
|
Infection
Inflammation/Immunology
|
|
Trypsin MS grade is a serine protease enzyme, and hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. Trypsin MS grade activates PAR2 and PAR4. Trypsin MS grade induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. Trypsin MS grade also promotes cell proliferation and differentiation. Trypsin MS grade can be used in the research of wound healing and neurogenic inflammation.
|
-
- HY-146001
-
|
Influenza virus-IN-4
|
Influenza Virus
|
Inflammation/Immunology
|
|
Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice.
|
-
- HY-111458
-
|
GSK2643943A
|
Deubiquitinase
|
Cancer
|
|
GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
|
-
- HY-124960
-
-
- HY-N8171
-
|
Lagotisoide D
10-O-[(E)-3,4-Dimethoxycinnamoyl]-catalpol
|
Others
|
Others
|
|
Lagotisoide D is a lridoid glycoside from Lagotis yunnanensis.
|
-
- HY-W127401
-
-
- HY-N7060
-
-
- HY-B0384
-
-
- HY-100713
-
-
- HY-153045
-
|
BAY-805
|
Deubiquitinase
|
Cancer
|
|
BAY-805 is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes.
|
-
- HY-124927
-
|
ARN14988
|
Others
|
Cancer
|
|
ARN14988 is a potent inhibitor of acid ceramidase (ACDase) (IC50=12.8 nM for the human enzyme).
|
-
- HY-D0149
-
-
- HY-P2822
-
|
Phosphoglycerate kinase
PGK
|
Endogenous Metabolite
|
Cancer
Infection
Endocrinology
|
Phosphoglycerate kinase (PGK), namely phosphoglycerate kinase, is a glycolytic enzyme commonly used in biochemical research. Phosphoglycerate kinase can catalyze the reversible transfer of phosphate groups from 1,3-bisphosphoglycerate (1,3-BPG) to ADP to generate 3-phosphoglycerate (3-PG) and ATP. At the same time, it can also participate in gluconeogenesis, catalyzing the opposite reaction to produce 1,3BPGA and ADP. Phosphoglycerate kinase is involved in energy metabolism, interaction with nucleic acid, tumor progression, cell death and virus replication and other related processes.
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-
- HY-U00459A
-
-
- HY-P4546
-
-
- HY-143433
-
|
Cdc7-IN-19
|
CDK
|
Cancer
|
|
Cdc7-IN-19 (compound 1-1) is a potent CDC7 inhibitor with an IC50 of 1.49 nM.
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-
- HY-130760
-
-
- HY-P1759
-
-
- HY-144800
-
|
FWM-1
|
SARS-CoV
|
Infection
|
|
FWM-1 is a potent SARS-COV-2 NSP13 helicase enzyme inhibitor with binding free energy equals -328.6 kcal/mol. FWM-1 effectively disrupts the binding of ATP to the SARS-COV2 helicase enzyme.
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-
- HY-N10420
-
|
Hinokinin
(-)-Hinokinin
|
HIV Protease
|
Infection
|
|
Hinokinin (Compound 1) is a compound isolated from the stems of Hypoestes aristate. Hinokinin exhibits moderate activity of HIV-1 protease enzyme.
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-
- HY-P1759B
-
-
- HY-N2074
-
|
Picrinine
|
Lipoxygenase
|
Inflammation/Immunology
|
|
Picrinine, an akuammiline alkaloid, is isolated from the leaves of Alstonia scholaris. Picrinine exhibits anti-inflammatory activity through inhibition of the 5-lipoxygenase enzyme.
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-
- HY-P1044
-
|
Spinorphin
LVV-hemorphin-4
|
Others
|
Neurological Disease
|
|
Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect.
|
-
- HY-113535
-
-
- HY-B2228
-
-
- HY-N7856
-
|
3-Oxooctadecanoic acid
3-Oxostearic acid
|
Others
|
Others
|
|
3-Oxooctadecanoic acid (3-Oxostearic acid) is a saturated fatty acid (SFA). 3-Oxooctadecanoic acid is an intermediate product in fatty acid biosynthesis and it was converted from malonic acid via the enzyme.
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-
- HY-N0680S5
-
-
- HY-117580
-
-
- HY-10827
-
-
- HY-117430
-
-
- HY-114304
-
|
COH000
|
E1/E2/E3 Enzyme
|
Cancer
|
|
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
|
-
- HY-N2383
-
|
Validamine
|
Glucosidase
|
Metabolic Disease
|
|
Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme.
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-
- HY-152148
-
|
JZP-MA-11
|
MAGL
|
Neurological Disease
|
|
JZP-MA-11 is a positron emission tomography (PET) ligand targeting the endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. JZP-MA-11 can cross the blood-brain barrier (BBB). [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP).
|
-
- HY-112862
-
|
Arg-AMS
|
Aminoacyl-tRNA Synthetase
|
Infection
|
|
Arg-AMS (compound 24) is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.
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-
- HY-136262
-
|
CRBN-6-5-5-VHL
|
PROTACs
|
Cancer
|
|
CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3.
|
-
- HY-147235
-
|
RIPK2-IN-2
|
RIP kinase
PROTACs
|
Infection
|
|
RIPK2-IN-2 (example 25) is a RIP2 kinase PROTAC inhibitor. RIPK2-IN-2 can block RIP2-dependent proinflammatory signaling, regulated RIP2 kinase activity in auto inflammatory diseases.
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-
- HY-141481
-
-
- HY-111532
-
|
(3R,4R)-A2-32-01
|
Bacterial
|
Infection
|
|
(3R,4R)-A2-32-01 (compound 24(R,R)), the (R,R)-enantiomer of A2-32-01, is a Staphylococcus aureus caseinolytic protease (SaClpP) inhibitor.
|
-
- HY-136614
-
|
H-Val-βNA
L-Valine β-naphthylamide
|
Others
|
Others
|
|
H-Val-βNA (L-Valine β-naphthylamide) can be used as an aminopeptidase and a Valine arylamidase substrate.
|
-
- HY-101681
-
-
- HY-B0263
-
-
- HY-U00459
-
|
GSK2850163
|
IRE1
|
Cancer
|
|
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
-
- HY-109040
-
|
Quilseconazole
VT-1129
|
Fungal
Cytochrome P450
|
Infection
|
|
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
|
-
- HY-U00459B
-
|
GSK2850163 hydrochloride
|
IRE1
|
Cancer
|
|
GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
-
- HY-W067056S1
-
|
Methyl(E)-cinnamate-d7
Methyl(E)-3-phenylpropenoate-d7
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Methyl(E)-cinnamate-d7 is the deuterium labeled Methyl (E)-cinnamate[1]. Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[2].
|
-
- HY-W067056S
-
|
Methyl (E)-cinnamate-d5
Methyl(E)-3-phenylpropenoate-d5
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Methyl (E)-cinnamate-d5 is the deuterium labeled Methyl (E)-cinnamate[1]. Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[2].
|
-
- HY-138067
-
|
SSAA09E2
|
SARS-CoV
|
Inflammation/Immunology
|
|
SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .
|
-
- HY-124781
-
|
ML406
|
Bacterial
Antibiotic
|
Infection
|
|
ML406 is a small molecule probe that shows anti-tubercular activity via M.tuberculosis BioA (DAPA synthase) enzyme inhibition with an IC50 of 30 nM. M.tuberculosis BioA is an enzyme involved in biotin biosynthesis in M.tuberculosis.
|
-
- HY-108321
-
-
- HY-U00041
-
-
- HY-B2220
-
|
Cellulase
|
Others
|
Others
|
|
Cellulase is an enzyme catalyzing the hydrolysis of certain linkages in cellulose and other carbohydrates.
|
-
- HY-18081
-
|
PF 750
|
FAAH
Autophagy
|
Metabolic Disease
|
|
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile.
|
-
- HY-18948
-
|
GSK321
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
GSK321 is a potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia.
|
-
- HY-110079
-
|
TNP
|
Others
|
Cancer
|
|
TNP is a cell-permeable inhibitor of IP6K1 and IP3K, with IC50 values of 0.55 µM and 10.2 µM for IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes.
|
-
- HY-B0655
-
-
- HY-16450
-
-
- HY-P1068
-
|
Lysozyme
Muramidase
|
Bacterial
|
Infection
|
|
Lysozyme is an antimicrobial enzyme produced by animals that forms part of the innate immune system.
|
-
- HY-W14549
-
|
D-(+)-Cellotriose
Cellotriose
|
Others
|
Others
|
|
D-(+)-Cellotriose (Cellotriose) is an oligosaccharide, it is an intermediate in the enzyme hydrolysis of cellulose.
|
-
- HY-N0680
-
-
- HY-P1004A
-
-
- HY-N0579
-
|
Fraxin
Fraxoside
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Fraxin isolated from Cortex Fraxini, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action, anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme.
|
-
- HY-W010378
-
|
D-Asparagine
H-D-Asn-OH
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Asparagine (H-D-Asn-OH) is a competitive inhibitor of L-Asparagine hydrolysis with a Ki value of 0.24 mM. D-Asparagine is a source of nitrogen for yeast strains. D-Asparagine is a good substrate for the external yeast asparaginase but is a poor substrate for the internal enzyme.
|
-
- HY-N6714
-
|
Alternariol
|
Topoisomerase
|
Cancer
Infection
|
|
Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes. Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties.
|
-
- HY-125776
-
|
Kresoxim-methyl
BAS 490 F
|
Fungal
Mitochondrial Metabolism
|
Infection
|
|
Kresoxim-methyl (BAS 490 F), a Strobilurin-based fungicide, inhibits the respiration at the complex III (cytochrome bc1 complex). Kresoxim-methyl binds to complex III from yeast with an apparent Kd of 0.07 μM proving a high affinity for this enzyme.
|
-
- HY-134354
-
|
pNP-ADPr
ADP-ribose-pNP
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Others
|
|
pNP-ADPr is a colorimetric substrate that used for the first continuous Poly(ADP-ribose) glycohydrolase (PARG) and ADP-ribosyl hydrolase 3 (ARH3) activity assays. pNP-ADPr can be used for the research of poly(ADP-ribose)polymerase (PARP) enzymes.
|
-
- HY-P0143
-
-
- HY-B0279
-
-
- HY-B2118
-
-
- HY-N2464
-
-
- HY-16710
-
|
GPDA
GPN; Glycylproline p-nitroanilide tosylate
|
Fluorescent Dye
|
Others
|
|
GPDA(Glycylproline p-nitroanilide tosylate) is the substarate of X-Prolyl dipeptidyl-aminopeptidase in the enzyme assay.
|
-
- HY-U00074
-
-
- HY-107337
-
-
- HY-152107
-
|
LRRK2-IN-7
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes.
|
-
- HY-117580S
-
-
- HY-N2472
-
|
Medicagenic acid
Castanogenin
|
Bacterial
|
Infection
|
|
Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes. Medicagenic acid (Castanogenin) has low enzyme inhibitory activities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE.
|
-
- HY-132987
-
|
Avibactam tomilopil
ARX-1796; AV-006
|
Bacterial
|
Infection
|
|
Avibactam tomilopil (ARX-1796, AV-006), an Avibactam proagent, is an orally bioavailable β-lactamase inhibitor. Avibactam has a spectrum of inhibition of class A and C β-lactamases, including ESBLs, AmpC and Klebsiella pneumoniae carbapenemase (KPC) enzymes.
|
-
- HY-76200
-
|
Voriconazole
UK-109496
|
Fungal
Bacterial
|
Infection
Cancer
|
|
Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
|
-
- HY-111518
-
|
JH-XI-10-02
|
PROTACs
CDK
|
Cancer
|
|
JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.
|
-
- HY-B0093
-
-
- HY-B1202
-
|
Alrestatin
AY-22284
|
Aldose Reductase
|
Endocrinology
|
|
Alrestatin is an inhibitor of aldose reductase, an enzyme involved in the pathogenesis of complications of diabetes mellitus, including diabetic neuropathy.
|
-
- HY-132606A
-
-
- HY-100312
-
-
- HY-B1202A
-
-
- HY-B0331A
-
-
- HY-107582
-
|
JW480
|
Others
|
Cancer
|
|
JW480 is a potent and selective inhibitor of a serine hydrolase enzyme KIAA1363.
|
-
- HY-145652
-
|
Narmafotinib
AMP-945
|
FAK
|
Cancer
|
|
Narmafotinib (AMP-945) is an inhibitor of the enzyme focal adhesion kinase (FAK).
|
-
- HY-A0043A
-
-
- HY-B0093A
-
-
- HY-A0043
-
-
- HY-13989
-
-
- HY-100615
-
-
- HY-18690A
-
-
- HY-146342
-
|
FAAH/MAGL-IN-3
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH/MAGL-IN-3 (Compound 10) is an irreversible fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) dual inhibitor with IC50 values of 179 and 759 nM against FAAH and MAGL, respectively. FAAH/MAGL-IN-3 shows low PAMPA (Parallel Artificial Membrane Permeability Assay) permeability.
|
-
- HY-150125
-
-
- HY-113951
-
-
- HY-146341
-
|
FAAH-IN-5
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH-IN-5 (Compound 7) is a relative selective, irreversible fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 10.5 nM. FAAH-IN-5 shows low PAMPA (Parallel Artificial Membrane Permeability Assay) permeability.
|
-
- HY-126362
-
|
ML266
|
Glucosidase
|
Others
|
|
ML266 is glucocerebrosidase (GCase) molecule chaperone with IC50 of 2.5 µM. ML266 binds to GCase and transports of the mutant protein to the lysosome, and resume the activity of GCase. ML266 dose not inhibit the GCase enzyme’s action. ML266 has the potential for the research of gaucher disease.
|
-
- HY-76200B
-
|
Voriconazole camphorsulfonate
UK-109496 camphorsulfonate
|
Fungal
Bacterial
|
Infection
|
|
Voriconazole (UK-109496) camphorsulfonate is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole camphorsulfonate exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
|
-
- HY-131312
-
|
Mutant IDH1-IN-6
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
|
-
- HY-139566
-
|
Abrucomstat
3-Nitroxypropanol; 3-NOP
|
Others
|
Others
|
|
Abrucomstat (3-Nitroxypropanol) acts as an enzyme inhibitor to decrease ruminal methanogenesis.
|
-
- HY-106446
-
-
- HY-16273A
-
-
- HY-B0331AS
-
-
- HY-146215
-
-
- HY-B0477
-
-
- HY-119689
-
|
Umibecestat
CNP520
|
Beta-secretase
|
Neurological Disease
|
|
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease.
|
-
- HY-129554
-
|
cis-9,10-Epoxystearic acid
cis-9,10-Epoxyoctadecanoic acid
|
Endogenous Metabolite
|
Others
|
|
cis-9,10-Epoxystearic acid (cis-9,10-Epoxyoctadecanoic acid) is an endogenous constituent in human blood and urine. cis-9,10-Epoxystearic acid (cis-9,10-Epoxyoctadecanoic acid) can be produced from oleic acid by enzymic and non-enzymic epoxidation.
|
-
- HY-100450
-
-
- HY-N7263
-
|
Galanthamine N-Oxide
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes.
|
-
- HY-147730
-
|
HDAC6-IN-8
|
HDAC
|
Cancer
|
|
A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.
|
-
- HY-111191A
-
|
(R)-ONO-2952
|
Others
|
Neurological Disease
|
|
(R)-ONO-2952 is a R-enantiomer of ONO-2952. ONO-2952 is a potent, selective and orally active TSPO antagonist with Kis of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes.
|
-
- HY-114507
-
|
Flumioxazin
Sumisoya; V-53482
|
Others
|
Others
|
|
Flumioxazin (Sumisoya) is an herbicide for use in soybean and peanut. Flumioxazin inhibits the enzyme protoporphyrinogen oxidase.
|
-
- HY-116023
-
-
- HY-P1488
-
-
- HY-N0913A
-
|
Isomaltotriose
|
Others
|
Others
|
|
Isomaltotriose is a sugar from enzymic hydrolyzates of the dextran from Leuconostoc mesenteroides NRRL B-512.
|
-
- HY-115772
-
-
- HY-124909A
-
|
FR054
|
Others
|
Cancer
|
|
FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect.
|
-
- HY-112861
-
-
- HY-D0146
-
|
Resorufin benzyl ether
BzRes; 7-Benzyloxyresorufin; 7-Benzyloxyphenoxazone
|
Fluorescent Dye
|
Others
|
|
Resorufin benzyl ether (BzRes), a fluorogenic enzyme substrate, can be used to detect CYP3A4 enzyme activity. Resorufin benzyl ether modified with a recognizing moiety boronate, can be used for ONOO - detection via a self-immolation mechanism. Ex/Em=530-570 nm/590 nm.
|
-
- HY-76200S
-
|
Voriconazole-d3
UK-109496-d3
|
Fungal
|
Infection
|
|
Voriconazole-d3 is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].
|
-
- HY-101790
-
-
- HY-N3247
-
-
- HY-131591
-
-
- HY-107994A
-
|
Aminoxyacetic acid
Carboxymethoxylamine; Aminooxyacetate
|
GABA Receptor
|
Cancer
|
|
Aminooxyacetic acid (Carboxymethoxylamine) is a malate-aspartate shuttle (MAS) inhibitor. Aminooxyacetic acid also inhibits the GABA degradating enzyme GABA-T.
|
-
- HY-112860
-
-
- HY-144799
-
-
- HY-18207
-
-
- HY-P1032
-
-
- HY-107318
-
-
- HY-101577
-
-
- HY-109059
-
-
- HY-D1208
-
-
- HY-W010538
-
-
- HY-16437
-
-
- HY-145933
-
|
BJJF078
|
Glutaminase
|
Inflammation/Immunology
|
|
BJJF078 is an aminopiperidine derivative. BJJF078 is a potent inhibitor of recombinant human and mouse Transglutaminase enzyme (TG2) activity, IC50 values of 41 and 54 nM, respectively. BJJF078 also inhibits the close related enzyme TG1, with an IC50 of 0.16 μM. BJJF078 can be used for Multiple sclerosis (MS) research.
|
-
- HY-112179
-
|
GSK180
|
Others
|
Inflammation/Immunology
|
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition.
|
-
- HY-147365
-
|
Acifluorfen-methyl
|
Others
|
Others
|
|
Acifluorfen-methyl is an inhibitor of the heme and chlorophyll biosynthetic enzyme protoporphyrinogen oxidase (Protox). Acifluorfen-methyl is a photobleaching herbicide.
|
-
- HY-107373
-
|
β-Chloro-L-alanine
L-β-Chloroalanine
|
Bacterial
|
Infection
|
|
β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.
|
-
- HY-P3142
-
-
- HY-13344A
-
-
- HY-B1093
-
-
- HY-107030
-
-
- HY-B0027
-
-
- HY-106816
-
-
- HY-132884
-
|
TTK inhibitor 3
|
Others
|
Cancer
|
|
TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC50 value of 3.0 nM.
|
-
- HY-113898
-
-
- HY-107994
-
|
Aminooxyacetic acid hemihydrochloride
Carboxymethoxylamine hemihydrochloride; Aminooxyacetate hemihydrochloride
|
GABA Receptor
|
Cancer
|
|
Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
|
-
- HY-B0231AS
-
-
- HY-A0116S
-
-
- HY-18206
-
-
- HY-108321S
-
-
- HY-13344
-
-
- HY-N0125
-
-
- HY-B0231BS
-
-
- HY-118517
-
|
α-Hydroxytamoxifen
(E)-α-Hydroxy tamoxifen; α-OHTAM
|
Drug Metabolite
|
Cancer
|
|
α-Hydroxytamoxifen is a metabolite of tamoxifen, reacts with DNA in the absence of metabolizing enzymes, and causes formation of DNA adducts.
|
-
- HY-112688
-
|
H-Arg-4MβNA
|
Others
|
Others
|
|
H-Arg-4MβNA is a substrate for cathepsin H, used for the detection of enzyme activity in gel electrophoresis.
|
-
- HY-141178
-
-
- HY-141181
-
-
- HY-W087383
-
-
- HY-133049
-
-
- HY-130146
-
-
- HY-130382
-
-
- HY-121507
-
-
- HY-123109
-
-
- HY-130554
-
-
- HY-141187
-
-
- HY-41921
-
-
- HY-130390
-
-
- HY-141159
-
-
- HY-141166
-
-
- HY-133230
-
-
- HY-130563
-
-
- HY-112559
-
-
- HY-141160
-
-
- HY-115414
-
-
- HY-130147
-
-
- HY-141161
-
-
- HY-141183
-
-
- HY-130374
-
-
- HY-133229
-
-
- HY-130137
-
-
- HY-141180
-
-
- HY-130389
-
-
- HY-130375
-
-
- HY-117045
-
-
- HY-126977
-
-
- HY-141189
-
-
- HY-141179
-
-
- HY-120587
-
-
- HY-141177
-
-
- HY-126891
-
-
- HY-141169
-
-
- HY-130378
-
-
- HY-130584
-
-
- HY-114670
-
-
- HY-141162
-
-
- HY-130373
-
-
- HY-130819
-
-
- HY-130380
-
-
- HY-130384
-
-
- HY-141188
-
-
- HY-113921
-
-
- HY-141168
-
-
- HY-140015
-
-
- HY-147944
-
|
Antimicrobial agent-4
|
Bacterial
Fungal
|
Infection
|
|
Antimicrobial agent-4 (compound 6a) is a potent antimicrobial agent. Antimicrobial agent-4 exhibits considerable activity against the microbial pathogens. Antimicrobial agent-4 delivers reliable toxicity to kill the bacteria and fungi. Antimicrobial agent-4 shows high binding energy value of −10.0 kcal/mole against the target enzyme.
|
-
- HY-129056
-
|
Melagatran
|
Thrombin
|
Cardiovascular Disease
|
|
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion.
|
-
- HY-101093
-
|
CA-170
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes.
|
-
- HY-76316
-
|
Bergaptol
5-Hydroxypsoralen; 4-Hydroxybergapten
|
Cytochrome P450
|
Cancer
|
|
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.
|
-
- HY-B0744
-
|
Eflornithine
DFMO; MDL71782; RMI71782; α-difluoromethylornithine
|
Parasite
|
Infection
Cancer
|
|
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-N0680S1
-
-
- HY-U00197
-
|
Tilmacoxib
JTE522; JTP19605; RWJ57504
|
COX
|
Inflammation/Immunology
|
|
Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.
|
-
- HY-128586A
-
-
- HY-B0331
-
-
- HY-N0680S2
-
-
- HY-B0744A
-
|
Eflornithine hydrochloride
DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride
|
Parasite
|
Infection
Cancer
|
|
Eflornithine hydrochloride is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-B0263S1
-
-
- HY-Y0801
-
-
- HY-B0242S1
-
|
Sulfanilamide-d4
Sulphanilamide-d4
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
|
-
- HY-D0091
-
-
- HY-128586
-
-
- HY-B0511S2
-
-
- HY-B0331B
-
-
- HY-B0882
-
|
Edrophonium chloride
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-131009
-
|
Fluorescein-NAD+
|
PARP
|
Others
|
|
Fluorescein-NAD+ is an alternative to radiolabeled NAD and a substrate for ADP-ribosylation. Fluorescein-NAD+ can be used in PARP assays by fluorescence microscopy. Extinction Coefficient: 262 nm.
|
-
- HY-143389
-
|
Cdc7-IN-14
|
CDK
|
Cancer
|
|
Cdc7-IN-14 (compound 82) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-14 has the potential for the research of cancer.
|
-
- HY-143387
-
|
Cdc7-IN-13
|
CDK
|
Cancer
|
|
Cdc7-IN-13 (compound 84) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-13 has the potential for the research of cancer.
|
-
- HY-143385
-
|
Cdc7-IN-12
|
CDK
|
Cancer
|
|
Cdc7-IN-12 (compound 1) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-12 shows antiproliferative activities with IC50 of 100-1000 nM in COLO205 cells. Cdc7-IN-12 has the potential for the research of cancer.
|
-
- HY-139979
-
|
USP5-IN-1
|
Deubiquitinase
|
Cancer
|
|
USP5-IN-1 (compound 64), a potent deubiquitinase USP5 inhibitor, binds to the USP5 ZnF-UBD with a KD of 2.8 μM. USP5-IN-1 is selective over nine proteins containing structurally similar ZnF-UBD domains. USP5-IN-1 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate.
|
-
- HY-146248
-
|
TFMU-ADPr
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Others
|
|
TFMU-ADPr is a general substrate for monitoring poly(ADP-ribose) glycohydrolase (PARG) activity. TFMU-ADPr can directly report on total PAR hydrolase activity via release of a fluorophore. TFMU-ADPr has excellent reactivity, generality, stability, and usability. TFMU-ADPr is a versatile tool for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes.
|
-
- HY-18054
-
|
BVT 2733
|
11β-HSD
|
Inflammation/Immunology
|
|
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.
|
-
- HY-128369
-
|
Acid Yellow 36
Metanil Yellow
|
Cytochrome P450
|
Others
|
|
Acid Yellow 36 (Metanil Yellow) is an azo dye and a pH indicator. Acid Yellow 36 changes its color from red at pH 1.2 to yellow at pH 2.3. Acid Yellow 36 is used in the leather, paper and textile industries. Acid Yellow 36 acts as a bifunctional inducer of specific isozymes of P-450 and cytosolic enzymes. Storage: protect from light.
|
-
- HY-122591
-
-
- HY-N0356
-
|
(-)-Catechin gallate
(-)-Catechin 3-gallate; (-)-Catechin 3-O-gallate
|
COX
|
Cancer
|
|
(-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of COX-1 and COX-2 enzymes.
|
-
- HY-B0511S
-
-
- HY-U00171
-
|
SQ28603
SQ28,603; Squibb 28603
|
Neprilysin
|
Metabolic Disease
|
|
SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).
|
-
- HY-N0680S
-
-
- HY-107337S
-
-
- HY-18206A
-
-
- HY-15930C
-
|
TMB monosulfate
BM blue monosulfate; Sure Blue TMB monosulfate
|
Fluorescent Dye
|
Others
|
|
TMB monosulfate is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualizing reagent used in enzyme-linked immunosorbent assays (ELISA).
|
-
- HY-P1244
-
-
- HY-N6667
-
|
Glucovanillin
|
Others
|
Others
|
|
Glucovanillin extracted from Vanilla planifolia Andrews and simultaneously transformed to vanillin by a combination of enzyme activities involving cell wall degradation and glucovanillin hydrolysis.
|
-
- HY-125112
-
-
- HY-B0511S1
-
-
- HY-107383
-
-
- HY-10825
-
-
- HY-B0279S
-
-
- HY-P2616
-
-
- HY-132824
-
-
- HY-B0580A
-
-
- HY-101790A
-
-
- HY-N2071
-
|
Cedrol
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities.
|
-
- HY-13635A
-
|
Finasteride acetate
MK-906 acetate
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
|
-
- HY-150702
-
|
MAGLi 432
|
MAGL
|
Inflammation/Immunology
Neurological Disease
|
|
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
|
-
- HY-W003445
-
|
4-Bromo-3-hydroxybenzoic acid
|
Endogenous Metabolite
|
Neurological Disease
|
|
4-Bromo-3-hydroxybenzoic acid is a metabolite of Brocresine and a histidine decarboxylase (HDC) inhibitor with IC50s of 1 mM for both rat fetal and rat gastric HDC. 4-Bromo-3-hydroxybenzoic acid also inhibits aromatic-L-amino acid decarboxylase from hog kidney and rat gastric mucosa in vitro with IC50s of 1 mM for both enzymes.
|
-
- HY-P3632
-
|
[DAla2, DArg6] Dynorphin A, (1-13) (porcine)
DADAD
|
Opioid Receptor
|
Metabolic Disease
Neurological Disease
|
|
[DAla2, DArg6] Dynorphin A, (1-13) (porcine) (DADAD) is an opioid peptide (dynorphinl-13, DYN) derivative found in porcine pituitary extracts. DYN is highly potent at the peripheral opioid receptors GPI and MVD, but is readily and rapidly degraded in vivo. [DAla2, DArg6] Dynorphin A, (1-13) (porcine) has some resistance to enzymatic cleavage and prevents peptide cleavage by enzymes.
|
-
- HY-13635
-
|
Finasteride
MK-906
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
|
-
- HY-15930A
-
|
TMB dihydrochloride
BM blue dihydrochloride; Sure Blue TMB dihydrochloride
|
Fluorescent Dye
|
Others
|
|
TMB dihydrochloride (BM blue dihydrochloride) is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualising reagent used in enzyme-linked immunosorbent assays (ELISA).
|
-
- HY-138126A
-
|
Dansyl-Tyr-Val-Gly TFA
|
Others
|
Neurological Disease
|
|
Dansyl-Tyr-Val-Gly TFA is a substrate of peptidylglycine monooxygenase (PHM). Peptidylglycine monooxygenase is an essential enzyme for the posttranslational amidation of neuroendocrine peptides.
|
-
- HY-10484
-
-
- HY-N9314
-
-
- HY-125826
-
-
- HY-114161
-
-
- HY-136211
-
-
- HY-N0680S3
-
-
- HY-103397A
-
-
- HY-18030
-
-
- HY-N9528
-
-
- HY-18733
-
-
- HY-16304
-
-
- HY-70062
-
-
- HY-15930
-
|
TMB
BM blue; Sure Blue TMB
|
Fluorescent Dye
|
Others
|
|
TMB (BM blue) is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualising reagent used in enzyme-linked immunosorbent assays (ELISA).
|
-
- HY-146248A
-
|
TFMU-ADPr triethylamine
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Others
|
|
TFMU-ADPr triethylamine is a general substrate for monitoring poly(ADP-ribose) glycohydrolase (PARG) activity. TFMU-ADPr triethylamine can directly report on total PAR hydrolase activity via release of a fluorophore. TFMU-ADPr triethylamine has excellent reactivity, generality, stability, and usability. TFMU-ADPr triethylamine is a versatile tool for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes.
|
-
- HY-148044
-
|
UNC10201652
|
Bacterial
|
Infection
|
|
UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide (HY-126373) processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes.
|
-
- HY-114158A
-
|
Pronase E (Activity ≥ 4000 U/mg)
Pronase (Activity ≥ 4000 U/mg)
|
Others
|
Others
|
|
Pronase E (Activity ≥ 4000 U/mg) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
|
-
- HY-B0744B
-
|
Eflornithine hydrochloride hydrate
DFMO hydrochloride hydrate; MDL-71782 hydrochloride hydrate; RMI-71782 hydrochloride hydrate; α-difluoromethylornithine hydrochloride hydrate
|
Parasite
|
Cancer
|
|
Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride hydrate is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-W020215
-
-
- HY-109592
-
-
- HY-126233
-
-
- HY-B0279S1
-
-
- HY-145705
-
|
Pencitabine
|
DNA/RNA Synthesis
|
Cancer
|
|
Pencitabine (Pen) is an orally active anticancer agent. Pencitabine interferes with DNA synthesis and function by inhibiting multiple nucleotide-metabolizing enzymes and by misincorporation into DNA.
|
-
- HY-W014120
-
|
Thianthrene
|
Others
|
Infection
|
|
Thianthrene, a sulfur-containing heterocyclic compound, is a derivative of dithiin. Thianthrene can be used in the research of dermal infections, in which it interferes with enzyme and nucleic acid function.
|
-
- HY-P4584
-
|
TRH-βNA
|
Biochemical Assay Reagents
|
Others
|
|
TRH-βNA is a substrate for determining the membrane TRH-deamidating enzyme (TRH-DE) activity and membrane pyroglutamyl aminopeptidase II (PPII) activity.
|
-
- HY-W011165
-
|
L-Lysyl-L-lysine dihydrochloride
Lysyllysine dihydrochloride
|
Others
|
Others
|
|
L-Lysyl-L-lysine (Lysyllysine) dihydrochloride is an enzyme cleavable basic amino acid. L-Lysyl-L-lysine dihydrochloride can be used for delivering multiple biologically active peptides.
|
-
- HY-N7195
-
|
12-Deoxywithastramonolide
|
Others
|
Others
|
|
12-Deoxywithastramonolide is a principle bioactive compound found in ashwagandha (W. somnifera). 12-Deoxywithastramonolide possesses antioxidant and enzyme inhibitory effects.
|
-
- HY-114161A
-
-
- HY-N1616
-
|
1β-Hydroxyeuscaphic acid
|
Apoptosis
|
Others
|
|
1β-Hydroxyeuscaphic acid has significant hepatoprotective activity by lowering the leakage of intracellular enzymes, reducing the oxidation of proteins and decreasing the incidence of apoptosis.
|
-
- HY-N2165
-
-
- HY-119847
-
|
Abafungin
BAY-W-6341
|
Fungal
|
Infection
|
|
Abafungin, a antifungal agent, inhibitis the transmethylation at the C-24 position of the sterol side chain, catalyzed by the enzyme sterol-C-24-methyltransferase.
|
-
- HY-N4090
-
-
- HY-15345
-
|
Tetrahydrouridine dihydrate
THU dihydrate; NSC-112907 dihydrate
|
Others
|
Cancer
|
|
Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
|
-
- HY-N3513
-
|
Mulberrin
Kuwanon C
|
Others
|
Cardiovascular Disease
|
|
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
|
-
- HY-N0548
-
|
α-Angelica lactone
|
Gutathione S-transferase
|
Cancer
|
|
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes.
|
-
- HY-139659
-
|
ARD-61
|
PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
|
Cancer
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice.
|
-
- HY-116872
-
|
MAC13772
|
Bacterial
|
Infection
|
|
MAC13772 is a potent inhibitor of the enzyme BioA (IC50=250 nM), the antepenultimate step in biotin biosynthesis. MAC13772 is a novel antibacterial compound.
|
-
- HY-112305
-
|
AZ32
|
ATM/ATR
|
Cancer
|
|
AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
|
-
- HY-132886
-
-
- HY-W010991
-
-
- HY-117281
-
-
- HY-106887
-
|
SCH 32615
|
Others
|
Neurological Disease
|
|
SCH 32615 is an enkephalinase (the enzymes responsible for the degradation of endogenous enkephalins) inhibitor. SCH 32615 can enhance surgery- and pregnancy-induced analgesia in mice.
|
-
- HY-114158
-
|
Pronase E (Activity ≥ 7000 U/g)
Pronase (Activity ≥ 7000 U/g)
|
Others
|
Others
|
|
Pronase E (Activity ≥ 7000 U/g) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
|
-
- HY-137840
-
|
Hippuryl-L-phenylalanine
|
Carboxypeptidase
|
Cancer
|
|
Hippuryl-L-phenylalanine is a substrate of carboxypeptidase. Carboxypeptidase is a protease enzyme that related with obesity, epilepsy and neurodegeneration. Hippuryl-L-phenylalanine can be used for the determination of carboxypeptidase activity.
|
-
- HY-15345A
-
|
Tetrahydrouridine
THU; NSC-112907
|
Others
|
Cancer
|
|
Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
|
-
- HY-U00373
-
-
- HY-111421
-
-
- HY-147361
-
|
LDCA
|
Apoptosis
Lactate Dehydrogenase
|
Cancer
|
|
LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression.
|
-
- HY-100796
-
-
- HY-135005
-
-
- HY-127146
-
|
Platensimycin
|
Antibiotic
Bacterial
|
|
|
Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
|
-
- HY-13635S
-
|
Finasteride-d9
MK-906-d9
|
5 alpha Reductase
|
Cancer
|
|
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
|
-
- HY-139409
-
-
- HY-143294
-
|
sEH inhibitor-2
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
sEH inhibitor-2 (compound 5l) is an orally active (predicted percentage absorption: 71.2-88.4%) soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 0.9 nM. sEH inhibitor-2 can maintain epoxyeicosatrienoic acids (EETs) serum level in high concentrations. sEH inhibitor-2 can be used in study of cardiovascular protection.
|
-
- HY-100640
-
-
- HY-107910
-
|
Hyaluronidase
Hyaluronate 4-glycanohydrolase; Hyaluronoglucosaminidase
|
Others
|
Others
|
|
Hyaluronidase (Hyaluronate 4-glycanohydrolase; Hyaluronoglucosaminidase) is a naturally occurring enzyme that depolymerizes hyaluronic acid by cleavage of glycosidic bonds and has been utilized in ophthalmic surgery.
|
-
- HY-W048449
-
|
L-Biotin
|
Others
|
Metabolic Disease
|
|
L-Biotin, also known as biotin, is a water-soluble vitamin that is an essential cofactor in the carboxylation of several enzymes. L-Biotin is involved in fatty acid synthesis and amino acid metabolism.
|
-
- HY-N6739
-
-
- HY-145326
-
|
Antibacterial agent 67
|
Fungal
|
Others
|
|
Antibacterial agent 67 (IC50 = 0.03 μM) has a great enzyme-inhibiting activity increase toward succinate dehydrogenase in comparison with fluxapyroxad (IC50 = 4.40 μM).
|
-
- HY-B1368
-
|
Fenclonine
4-Chloro-DL-phenylalanine; PCPA; CP-10188
|
Tryptophan Hydroxylase
|
Cancer
Neurological Disease
|
|
Fenclonine is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine can be used in carcinoid syndrome research.
|
-
- HY-100365
-
|
Remetinostat
SHP-141
|
HDAC
|
Cancer
|
|
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma.
|
-
- HY-50737
-
|
DUB-IN-3
|
Deubiquitinase
|
Cancer
|
|
DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor extracted from reference compound 22c with an IC50 of 0.56 μM for USP8.
|
-
- HY-125857
-
-
- HY-W040073
-
|
Nifurtimox
|
Parasite
Lactate Dehydrogenase
|
Cancer
Infection
|
|
Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
|
-
- HY-12988
-
|
C527
|
Deubiquitinase
|
Cancer
|
|
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
|
-
- HY-113081
-
|
1-Methyladenosine
|
Endogenous Metabolite
|
Others
|
|
1-Methyladenosine is an RNA modification originating essentially from two different reaction types, one catalyzed by enzymes and the other the result of the reaction of RNA with certain alkylating agents.
|
-
- HY-145197
-
-
- HY-112734
-
-
- HY-N10860
-
-
- HY-P1853
-
-
- HY-N6702
-
-
- HY-119737
-
|
Chlorsulfuron
|
Acetolactate Synthase (ALS)
|
Metabolic Disease
|
|
Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase.
|
-
- HY-101255
-
|
ODQ
|
Guanylate Cyclase
Apoptosis
|
Cancer
|
|
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
|
-
- HY-109066
-
-
- HY-P1244A
-
-
- HY-125999
-
|
EPI-589
|
Others
|
Neurological Disease
|
|
EPI-589, a quinone derivative, is a safe and well tolerated oxidoreductase enzyme inhibitor. EPI-589 has the potential for the treatment of amyotrophic lateral sclerosis (ALS).
|
-
- HY-P2329
-
-
- HY-B2193
-
|
α-Amylase
|
Others
|
Others
|
|
α-Amylase is a hydrolase enzyme that catalyses the hydrolysis of internal α-1, 4-glycosidic linkages in starch to yield products like glucose and maltose.
|
-
- HY-148699
-
-
- HY-148700
-
-
- HY-N0529
-
-
- HY-N10361
-
|
Drupanin
|
Others
|
Cancer
|
|
Drupanin is a compound isolated from green propolis. Drupanin can selectively inhibit the AKR1C3 enzyme. Drupanin has the potential for the research of breast cancer.
|
-
- HY-B1189
-
-
- HY-18206S
-
-
- HY-N0125S
-
|
Diosmetin-d3
|
Cytochrome P450
|
Cancer
|
|
Diosmetin-d3 is the deuterium labeled Diosmetin. Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
|
-
- HY-N6805
-
|
Isoeugenol acetate
Acetyl isoeugenol
|
Cholinesterase (ChE)
|
Cancer
Inflammation/Immunology
|
|
Isoeugenol acetate (Acetyl isoeugenol), an essential oil constituent of nutmeg, clove, and cinnamon, shows excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes (IC50=77 nM; Ki=16 nM), α-glycosidase (IC50=19.25 nM; Ki=21 nM), and α-amylase (IC50=411.5 nM). Isoeugenol acetate is used medical and cosmetics industries for its antioxidant, anticancer, antimicrobial and anti-inflammatory properties.
|
-
- HY-B0592S
-
-
- HY-144681
-
|
LY3372689
|
Tau Protein
|
Neurological Disease
|
|
LY3372689 (Formulaic Ia) is an orally active O-GlcNAcase (OGA) enzyme inhibitor. LY3372689 can be used for tauopathies research, including Alzheimer’s disease.
|
-
- HY-W028047
-
-
- HY-Y1422
-
|
Triacylglycerol lipase
|
Others
|
Metabolic Disease
|
|
Triacylglycerol lipase is an enzyme that preferentially hydrolyzes the outer links of triacylglycerols and acts only on the water-lipid interface. Pancreatic triacylglycerol lipase is the single most important determinant of lipid absorption.
|
-
- HY-B0378A
-
-
- HY-B0329
-
|
Isoniazid
INH; Isonicotinic acid hydrazide; Isonicotinic hydrazide
|
Bacterial
Autophagy
Mitophagy
Antibiotic
|
Infection
|
|
Isoniazid (INH) is a proagent and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity.
|
-
- HY-18062S
-
|
Pyrimethamine-d3
|
Antifolate
Parasite
|
Infection
|
|
Pyrimethamine-d3 is the deuterium labeled Pyrimethamine. Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR)[1][2].
|
-
- HY-B0882S
-
|
Edrophonium-d5 chloride
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-18169
-
|
MUT056399
Fab-001
|
Bacterial
|
Infection
|
|
MUT056399 (Fab-001) is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively.
|
-
- HY-W012595A
-
|
trans-Benzylideneacetone
trans-Benzalacetone
|
Phospholipase
|
Inflammation/Immunology
|
|
trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). trans-Benzylideneacetone is an immunosuppressant.
|
-
- HY-140656F
-
|
Biotin-PEG-Biotin (MW 20000)
|
Fluorescent Dye
|
Others
|
|
Biotin-PEG-Biotin (MW 20000) is a biotin labeled PEG derivative. Biotin is an enzyme co-factor, can be used for labeling protein; PEG is a hydrophilic and water-soluble polymer with low toxicity.
|
-
- HY-N2266
-
-
- HY-112157
-
-
- HY-W016813
-
|
trans-Aconitic acid
|
Endogenous Metabolite
|
Others
|
|
trans-Aconitic acid is present in normal human urine, and it has been suggested that is present in larger amounts with Reye's syndrome and organic aciduria. trans-Aconitic acid is a substrate of enzyme trans-aconitate 2-methyltransferase.
|
-
- HY-W009993
-
|
3,4-Methylenedioxycinnamic acid
|
Others
|
Others
|
|
3,4-Methylenedioxycinnamic acid is an inhibitor of the phenylpropanoid enzyme 4-hydroxycinnamoyl-CoA ligase. 3,4-Methylenedioxycinnamic acid increases the formation of soluble phenolics in particular of vanillic acid.
|
-
- HY-13592
-
|
HDAC-IN-7
Chidamide impurity
|
HDAC
|
Cancer
|
|
HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
|
-
- HY-12493A
-
-
- HY-D1529
-
-
- HY-144739
-
-
- HY-N9508
-
|
Perilla ketone
|
Others
|
Inflammation/Immunology
|
|
Perilla ketone is a naturally occurring xenobiotic compound. Perilla ketone is activated by pulmonary P450 cytochrome enzymes in the lung, resulting in severe pulmonary damage and development of diffuse pulmonary edema.
|
-
- HY-100283
-
|
CGS 15435
|
Others
|
Inflammation/Immunology
Endocrinology
|
|
CGS 15435, a potent thromboxane (TxA2) synthetase inhibitor with an IC50 of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI2 synthetase and lipoxygenase enzymes.
|
-
- HY-D1678
-
-
- HY-12493B
-
-
- HY-P4654
-
-
- HY-145302
-
|
Mycobactin-IN-2
|
Bacterial
|
Infection
|
|
Mycobactin-IN-2 (compound 49) is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-2 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway.
|
-
- HY-144741
-
-
- HY-18341B
-
-
- HY-140902A
-
-
- HY-152113
-
|
AChE/BChE/MAO-B-IN-3
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE/MAO-B-IN-3, an indan-1-one derivative, is a potent MAO-B inhibitor with an IC50 of 0.0359 μM for human MAO-B. AChE/BChE/MAO-B-IN-3 is a potent AChE and BChE enzyme inhibitor, with IC50s of 0.0473 μM and 0.0782 μM for human AChE and BChE enzyme, respectively. AChE/BChE/MAO-B-IN-3 shows significant antioxidant activity and has the potential for Alzheimer's disease (AD) research.
|
-
- HY-148825
-
-
- HY-10865
-
|
LY2183240
|
FAAH
Autophagy
|
Neurological Disease
|
|
LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively [3].
|
-
- HY-130241
-
|
Reverse transcriptase-IN-1
|
HIV
|
Infection
|
|
Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme.
|
-
- HY-114424A
-
-
- HY-D1257
-
|
Msr-Ratio
Msr-green
|
Fluorescent Dye
|
Others
|
|
Msr-Ratio (Msr-green) is a ratiometric fluorescent probe of methionine sulfoxide reductase (λex=375 nm, λem=550 nm). Msr-Ratio is used for monitoring the enzyme activity in vitro and in live cells.
|
-
- HY-18205
-
-
- HY-122832
-
|
ABC99
|
Wnt
|
Cancer
|
|
ABC99 is an N-hydroxyhydantoin (NHH) carbamate that selectively inhibits the Wnt-deacylating enzyme NOTUM (IC50=13 nM). ABC99 preserves Wnt3A signaling in the presence of NOTUM.
|
-
- HY-107352
-
