proteolytic degradation

By Targets:	Akt (1) Androgen Receptor (1) Apoptosis (3) Autophagy (1) Biochemical Assay Reagents (1) Btk (1) Caspase (2) CFTR (2) Deubiquitinase (1) EGFR (1) Endogenous Metabolite (2) GLUT (1) HIF/HIF Prolyl-Hydroxylase (1) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (1) PARP (3) PROTACs (2) Reference Standards (1) TGF-beta/Smad (1) TGF-β Receptor (1)
By Research Areas:	Cancer (8) Cardiovascular Disease (1) Neurological Disease (1)

Targets Recommended: Proteolytic Enzyme

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-E70231

Thrombin-like enzyme	Others	Cardiovascular Disease
Thrombin-like enzyme is a proteolytic enzyme extraction of Agkistrodon halys venom. Thrombin-like enzyme can be used for degradation of fibrinogen. Thrombin-like enzyme can exacerbate myosin-induced EAM (experimental autoimmune myositis). Thrombin-like enzyme can be used for degradation of fibrinogen. Thrombin-like enzyme is commonly used for research of acute ischemic cerebrovascular disease, thromboangiitis obliterans, deep phlebitis and sudden deafness .

HY-156106

VHL-IN-1	Ligands for E3 Ligase HIF/HIF Prolyl-Hydroxylase	Cancer
VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) .

HY-149428

AD4 1 Publications Verification	PROTACs	Cancer
AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC₅₀: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy .

HY-137677B

GTPγS tetralithium Guanosine 5'-[γ-thio]triphosphate tetralithium	GLUT	Others
GTPγS (tetralithium) (Guanosine 5'-[γ-thio]triphosphate (tetralithium)) is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS (tetralithium) to couple with G- protein α, to study its effect on kinase activity. GTPγS (tetralithium) acts as a component of lysis buffer .

HY-136528

RA-9	Deubiquitinase Apoptosis	Cancer
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .

HY-N6818

5,7,4'-Trimethoxyflavone 1 Publications Verification MTF	Apoptosis Caspase PARP Endogenous Metabolite CFTR	Cancer
5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC₅₀ is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress .

HY-P10110

retro-inverso TAT-Beclin 1 (D-amino acid)	Autophagy	Neurological Disease
retro-inverso TAT-Beclin 1 D-amino acid is has higher activity and resistance to proteolytic degradation in vivo compared to L-amino acids peptide. TAT-Beclin 1 can induce autophagy in peripheral tissues in adult mice as well as in the central nervous system of neonatal mice .

HY-141486A

PROTAC PARP/EGFR ligand 1	PARP EGFR Ligands for Target Protein for PROTAC	Others
PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology .

HY-P10661

L-KYFIL	Biochemical Assay Reagents	Others
L-KYFIL is a pentapeptide that is amorphous on its own. When mixed with D-KYFIL, it transforms from fibrous hydrogels into plate-like networks, resulting in changes in mechanical properties and forming a crystalline state. The mixture can protect L-KYFIL from proteolytic degradation. L-KYFIL can be used to study stereocomplexation behavior of peptide sequences and in the development of biomaterials .

HY-161398

TGFβRII-IN-3	TGF-β Receptor TGF-beta/Smad	Cancer
TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC₅₀ = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research .

HY-175455

LYA914	PROTACs Androgen Receptor Akt	Cancer
LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .

HY-N6818R

5,?7,?4'-?Trimethoxyflavone (Standard) MTF (Standard)	Reference Standards Apoptosis Caspase PARP Endogenous Metabolite CFTR	Cancer
5,?7,?4'-Trimethoxyflavone (Standard) is the analytical standard of 5,?7,?4'-Trimethoxyflavone. This product is intended for research and analytical applications. 5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC₅₀ is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress .

HY-179562

BTK degrader-2	Btk	Cancer
BTK degrader-2 (Example 2) is a BTK dual-functional degrading agent, which causes the degradation of BTK through the ubiquitin-proteasome pathway. BTK degrader-2 can be used for the study of B-cell-related diseases .

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library	3,470 compounds
Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression. Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival. HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation. MCE offers a unique collection of 3,470 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Oxygen Sensing Compound Library

3,470 compounds

Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

MCE offers a unique collection of 3,470 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Cat. No.	Product Name	Target	Research Area

HY-P10110

retro-inverso TAT-Beclin 1 (D-amino acid)	Autophagy	Neurological Disease
retro-inverso TAT-Beclin 1 D-amino acid is has higher activity and resistance to proteolytic degradation in vivo compared to L-amino acids peptide. TAT-Beclin 1 can induce autophagy in peripheral tissues in adult mice as well as in the central nervous system of neonatal mice .

HY-P10661

L-KYFIL	Biochemical Assay Reagents	Others
L-KYFIL is a pentapeptide that is amorphous on its own. When mixed with D-KYFIL, it transforms from fibrous hydrogels into plate-like networks, resulting in changes in mechanical properties and forming a crystalline state. The mixture can protect L-KYFIL from proteolytic degradation. L-KYFIL can be used to study stereocomplexation behavior of peptide sequences and in the development of biomaterials .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6818

5,7,4'-Trimethoxyflavone 1 Publications Verification MTF	Flavonoids Classification of Application Fields Flavones Source classification Kaempferia parviflora Wall. ex Baker Plants Disease Research Fields Zingiberaceae Cancer	Apoptosis Caspase PARP Endogenous Metabolite CFTR
5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC₅₀ is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress .

HY-N6818R

5,?7,?4'-?Trimethoxyflavone (Standard) MTF (Standard)	Flavonoids Flavones Source classification Kaempferia parviflora Wall. ex Baker Plants Zingiberaceae	Reference Standards Apoptosis Caspase PARP Endogenous Metabolite CFTR
5,?7,?4'-Trimethoxyflavone (Standard) is the analytical standard of 5,?7,?4'-Trimethoxyflavone. This product is intended for research and analytical applications. 5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC₅₀ is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress .

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