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Results for "

selective degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AAK1 (1) Acetolactate Synthase (ALS) (1) ADC Payload (1) Adrenergic Receptor (2) Akt (18) Aminopeptidase (1) Amyloid-β (4) Anaplastic lymphoma kinase (ALK) (3) Androgen Receptor (9) Annexin A (1) Antibiotic (2) Apoptosis (80) Aryl Hydrocarbon Receptor (1) ASK1 (2) ATM/ATR (2) ATP Synthase (1) Aurora Kinase (7) AUTACs (1) Autophagy (15) AUTOTACs (2) Bacterial (4) Bcl-2 Family (8) BCL6 (4) Bcr-Abl (2) Biochemical Assay Reagents (1) BTB/POZ Family (1) Btk (5) c-Myc (3) Cadherin (1) CaMK (1) Cannabinoid Receptor (1) Casein Kinase (2) Caspase (6) Cathepsin (3) CDK (33) Cholecystokinin Receptor (1) ClpP (1) CRM1 (1) Cryptochrome (1) Cyclic GMP-AMP Synthase (1) Cyclophilin (1) Cytochrome P450 (1) Deubiquitinase (7) Dipeptidyl Peptidase (11) DNA Methyltransferase (1) DNA/RNA Synthesis (8) Dopamine Receptor (1) Drug Intermediate (1) Drug Metabolite (2) E1/E2/E3 Enzyme (5) E3 Ligase Ligand-Linker Conjugates (9) Early 2 Factor (E2F) (1) EGFR (17) Endogenous Metabolite (20) Endonuclease (1) Ephrin Receptor (2) Epigenetic Reader Domain (54) Epoxide Hydrolase (1) ERK (18) Estrogen Receptor/ERR (46) Eukaryotic Initiation Factor (eIF) (1) FAK (5) Fat Mass and Obesity-associated Protein (FTO) (1) Ferroptosis (4) FGFR (3) FKBP (8) FLT3 (9) Fluorescent Dye (1) Fungal (1) GLP Receptor (10) Glutaminase (1) Glutathione Peroxidase (2) GSK-3 (3) HCV (1) HDAC (20) Hexokinase (1) HIF/HIF Prolyl-Hydroxylase (1) Histone Acetyltransferase (7) Histone Demethylase (1) Histone Methyltransferase (11) HIV (1) HSP (10) IAP (4) IFNAR (3) IKK (1) IKZF Family (7) Influenza Virus (1) Insulin Receptor (1) Interleukin Related (6) IRAK (6) Isotope-Labeled Compounds (12) Itk (1) JAK (8) Keap1-Nrf2 (2) Ligands for E3 Ligase (17) Ligands for Target Protein for PROTAC (17) LIM Kinase (LIMK) (2) Liposome (1) LRRK2 (2) LYTACs (1) MALT1 (1) MAP4K (1) MDM-2/p53 (5) MEK (2) METTL3 (2) MHC (1) Microtubule/Tubulin (1) Mitochondrial Metabolism (1) Mitosis (1) MMP (2) MNK (1) Molecular Glues (38) Monoamine Oxidase (2) mTOR (1) Myosin (2) Na+/K+ ATPase (1) NEKs (1) Neprilysin (2) NF-κB (4) NOD-like Receptor (NLR) (1) P-glycoprotein (1) p38 MAPK (6) p62 (1) PAI-1 (1) PAK (2) Parasite (3) PARP (8) PD-1/PD-L1 (5) PDGFR (1) PDHK (1) PGE synthase (1) Phosphatase (4) Phosphodiesterase (PDE) (10) Photosystem II (1) PI3K (5) PI5P4K (1) PIKfyve (1) PIN1 (1) PKA (10) Polo-like Kinase (PLK) (2) Potassium Channel (5) Prolyl Endopeptidase (PREP) (1) PROTAC Linkers (12) PROTAC-Linker Conjugates for PAC (1) PROTACs (279) Proteasome (2) Proteolytic Enzyme (1) PTEN (1) Raf (2) RAR/RXR (1) Ras (5) Reactive Oxygen Species (ROS) (3) Reference Standards (11) RET (2) RIP kinase (3) ROR (1) Salt-inducible Kinase (SIK) (1) SDCBP (1) Ser/Thr Kinase (1) Ser/Thr Protease (1) SGK (1) Sirtuin (1) Small Interfering RNA (siRNA) (2) SNIPERs (1) Src (3) STAT (17) STING (1) Survivin (2) SWI/SNF Complex (1) TAM Receptor (2) Target Protein Ligand-Linker Conjugates (2) TGF-beta/Smad (1) TGF-β Receptor (1) TNF Receptor (3) Toll-like Receptor (TLR) (3) Topoisomerase (1) Transmembrane Glycoprotein (1) Trk Receptor (2) TRP Channel (1) Tyrosinase (1) ULK (1) VEGFR (2) WDR5 (2) Wee1 (1) Wnt (5) YAP (1) YTHDF (1) α-synuclein (5) β-catenin (6)
By Research Areas:	Cancer (462) Cardiovascular Disease (10) Endocrinology (5) Infection (6) Inflammation/Immunology (35) Metabolic Disease (30) Neurological Disease (29)
Click Chemistry:	DBCO (1) PROTAC Synthesis (8) Azide (5) Alkynes (5)
Oligonucleotides:	Cationic Lipids (1) siRNA drugs (2) siRNAs (2)

555

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-123911

dBET23	PROTACs Epigenetic Reader Domain	Cancer
dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC_50/5h of ~ 50 nM for BRD4_BD1 protein .

HY-132857A

ZXH-4-130 TFA 1 Publications Verification	PROTACs	Neurological Disease
ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN degradation at 10 nM in MM1.S cells .

HY-123058

Vps34-IN-4	PI3K Autophagy	Cancer
Vps34-IN-4 (compound 19) is a potent, selective, and orally active inhibitor of VPS34. Vps34-IN-4 inhibits the autophagy in vivo. Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components .

HY-115997

PROTAC HSP90 degrader BP3	PROTACs HSP	Cancer
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC₅₀=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-145341

GNE-149	Estrogen Receptor/ERR	Cancer
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC₅₀=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .

HY-130612

PROTAC BRD2/BRD4 degrader-1	Epigenetic Reader Domain PROTACs	Cancer
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .

HY-175144

KRASG12D-IN-6	Ligands for Target Protein for PROTAC Ras	Cancer
KRASG12D-IN-6 is a PROTAC target protein ligand that can be used to synthesize CH091138 (HY-175025). CH091138 is a potent and selective KRASG12D PROTAC degrader with anti-tumor activity .

HY-175025

CH091138	PROTACs Ras Apoptosis	Cancer
CH091138 is a potent and selective KRASG12D PROTAC degrader with DC₅₀s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS ^WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)) .

HY-101119

GLL398	Estrogen Receptor/ERR	Cancer
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC₅₀ value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC₅₀=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.

HY-123971

HDAC6 degrader-4	HDAC PROTACs	Cancer
HDAC6 degrader-4 is a PROTAC and a selective HDAC6 degrader consists of a non-selective HDAC inhibitor and thalidomide-type E3 ligase ligand. HDAC6 degrader-4 can be used for cancer research .

HY-103628

PROTAC CDK9 Degrader-1 2 Publications Verification	PROTACs CDK	Cancer
PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.

HY-142662

PROTAC IRAK3 degrader-1	PROTACs IRAK	Others
PROTAC IRAK3 degrade-1 (compound 23) is a potent and selective degrader of IRAK3 (IC₅₀ = 5 nM) .

HY-168965

BTK ligand 15	Ligands for Target Protein for PROTAC	Others
BTK ligand 15 is the target protein ligand of PROTAC BTK Degrader-13 (HY-168963). PROTAC BTK Degrader-13 can selectively degrade BTK .

HY-107425

MZ 1 20+ Cited Publications	PROTACs Epigenetic Reader Domain	Cancer
MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively .

HY-149969

ER degrader 4	Estrogen Receptor/ERR	Cancer
ER degrader 4 is a selective and orally active estrogen receptor degrader. ER degrader 4 has anti-tumor activity .

HY-162014

WDR5 degrader-1	PROTACs WDR5	Cancer
WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1 .

HY-142662A

PROTAC IRAK3 degrade-1 formic	PROTACs IRAK	Others
PROTAC IRAK3 degrade-1 (compound 23) formic is a potent and selective degrader of IRAK3 (IC₅₀=5 nM) .

HY-169274

PROTAC SMARCA2 degrader-23	PROTACs Epigenetic Reader Domain	Cancer
PROTAC SMARCA2 degrader-23 (Example 1) is a potent and selective PROTAC SMARCA2 degrader，with a DC₅₀ of <100 nM. PROTAC SMARCA2 degrader-23 has the potential for the research of cancer .

HY-168518

PROTAC CDK9 degrader-9	PROTACs CDK	Cancer
PROTAC CDK9 degrader-9 (compound 29) is a highly selective and efficient CDK9 degrader based on PROTAC technology. PROTAC CDK9 degrader-9 can be used in anti-cancer research .

HY-163920

PROTAC HDAC8 Degrader-1	PROTACs HDAC	Cancer
Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC₅₀ of 0.27 nM in A549 cells .

HY-164827

CDK2 degrader 3	CDK	Cancer
CDK2 degrader 3 can selectively degrade CDK2 and has anti-tumor activity .

HY-161692

ERα degrader 8	Estrogen Receptor/ERR	Cancer
ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC₅₀ value of 0.15 μM .

HY-144605

PROTAC EGFR degrader 3	EGFR PROTACs	Cancer
PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .

HY-139185

PROTAC ERRα Degrader-3 1 Publications Verification	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins .

HY-155582

BLK degrader 1	Src	Cancer
BLK degrader 1 (compound 9) is a selective degrader of B-lymphoid tyrosine kinase (BLK). BLK degrader 1 shows anticancer activity in several B-lymphoid cell lines .

HY-155102

PROTAC TG2 degrader-2	PROTACs Glutaminase	Cancer
PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with K_d > 100 μM. PROTAC TG2 degrader-2 inhibits the cell migration and decreases the level of TG2 in ovarian cancer cells. PROTAC TG2 degrader-2 can be used for ovarian cancer study .

HY-144624

PROTAC Axl Degrader 1	PROTACs TAM Receptor	Cancer
PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC₅₀ of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis .

HY-144627

PROTAC Axl Degrader 2	PROTACs TAM Receptor	Cancer
PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC₅₀ of 1.61 μM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis .

HY-174135

PROTAC HPK1 Degrader-4	PROTACs MAP4K	Cancer
PROTAC HPK1 Degrader-4 (compound E3) is a selective and orally active PROTAC HPK1 degrader with a DC₅₀ of 3.16 nM. PROTAC HPK1 Degrader-4 demonstrates >1000-fold selectivity over GLK. PROTAC HPK1 Degrader-4 promotes immune activation. PROTAC HPK1 Degrader-4 can be used for the study of colon cancer and lymphoma (Pink: ligand for target protein (HY-174355); Blue: ligand for E3 ligase CRBN (HY-45808); Black: Linker (HY-174356); Target protein ligand-linker Conjugate (HY-174357)) .

HY-177729

PROTAC BRD9 Degrader-9	Epigenetic Reader Domain PROTACs	Cancer
PROTAC BRD9 Degrader-9 is an efficient and selective targeting BRD9 PROTAC degrader. PROTAC BRD9 Degrader-9 does not cause significant cytotoxicity. PROTAC BRD9 Degrader-9 can be used for cancer research. (Pink: BRD9 Ligand (HY-107446); Blue: CRBN Ligand (HY-W877239))

HY-152227

PROTAC TYK2 degradation agent1	PROTACs JAK	Inflammation/Immunology
PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader. PROTAC TYK2 degradation agent1 has TYK2 degradation activity with DC₅₀ value of 14 nM. PROTAC TYK2 degradation agent1 can be used for the research of autoimmune disease .

HY-153582

ML 2-23	PROTACs Bcr-Abl	Cancer
ML 2-23 is a potent PROTAC BCR-ABL degrader. ML 2-23 is selectively degrade BCR-ABL in a proteasome-dependent manner in leukemia cells .

HY-169955A

WIZ degrader 8 TFA	Histone Acetyltransferase Molecular Glues	Cardiovascular Disease
WIZ degrader 8 (TFA) is the trifluoroacetic acid of WIZ degrader 8 (HY-169955). WIZ degrader 8 (compound 10) is a potent and selective degrader of the transcription factor WIZ, which can potently induce HbF expression. WIZ degrader 8 can lead to WIZ degradation and induce HbF expression, and has the potential to be an inhibitor of sickle cell disease .

HY-178161

HDAC degrader-2	HDAC Apoptosis	Cancer
HDAC degrader-2 is a selective HDAC degrader with a DC₅₀ values of 2.55 μM against HDAC1. HDAC degrader-2 effectively induces the degradation of HDAC1 and HDAC2, but has no significant effect on the degradation of HDAC3, 4, 6 and 8. HDAC degrader-2 exerts potent antiproliferative effects against MM.1S and MCF-7 cells. HDAC degrader-2 induces apoptosis in myeloma cells. HDAC degrader-2 can be used for the study of myeloma .

HY-169955

WIZ degrader 8	Histone Acetyltransferase Molecular Glues	Cardiovascular Disease
WIZ degrader 8 (compound 10) is a potent and selective degrader of the transcription factor WIZ, which can potently induce HbF expression. WIZ degrader 8 can lead to WIZ degradation and induce HbF expression, and has the potential to be an inhibitor of sickle cell disease .

HY-175767

PROTAC BRD4 Degrader-39	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC₅₀ value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))

HY-161616

ATR-IN-30	ATM/ATR	Cancer
ATR-IN-30 is a selective ATR ligand, and can be used for synthesis of ATR PROTACs, such as PROTAC ATR degrader-2 (HY-161615) .

HY-132194

ERα degrader-2	Estrogen Receptor/ERR	Cancer
ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC₅₀=17.1 nM), good degradation efficacy (EC₅₀=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER ⁺ breast cancer research .

HY-132862

ZXH-4-137	PROTACs	Cancer
ZXH-4-137 is a potent and selective CRBN degrader (PROTAC).

HY-146267

ERα degrader 5	Estrogen Receptor/ERR	Cancer
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC₅₀ of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .

HY-163814

CDK2 degrader 1	Molecular Glues CDK	Cancer
CDK2 degrader 1 (Compound 3) is a selective CDK2 molecular glue degrader with a D_max (CDK2) of > 80% and a K_i (CRBN) > 1 μM. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers .

HY-152134

HDAC6 degrader-3	HDAC PROTACs	Cancer
HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC₅₀ value of 19.4 nM. HDAC6 degrader-3 has IC₅₀s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin .

HY-168099

ERα degrader 10	Estrogen Receptor/ERR	Cancer
ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC₅₀ of 24.0 nM) and degradation ability (EC₅₀ of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer .

HY-148523

HQ005	Molecular Glues CDK	Cancer
HQ005 is a potent CCNK degrader with an DC₅₀ value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation .

HY-174870

PROTAC ERα Degrader-11	PROTACs Estrogen Receptor/ERR Apoptosis Fluorescent Dye	Cancer
PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .

HY-153425

PROTAC SMARCA2 degrader-2	PROTACs	Cancer
PROTAC SMARCA2 degrader-2 is a potent and selective SMARCA2/4 PROTAC degrader with an IC₅₀ of <0.1 μΜ in HeLa HiBiT assay. PROTAC SMARCA2 degrader-2 is extracted from patent WO2023287787A1 and has the potential for SMARCA4-related or deficient cancer research .

HY-153385

TMX1	Molecular Glues Epigenetic Reader Domain Apoptosis	Cancer
TMX1 is a BRD4 covalent molecular glue degrader. TMX1 selectively recruits DCAF16 to the BRD4BD2, leading to BRD4 degradation.

HY-176486

ER degrader 11	Estrogen Receptor/ERR	Cancer
ER degrader 11 (Compound 5) is an orally active, brain-penetrant and selective estrogen receptor (ER) degrader (ERα IC₅₀=1.6 nM). ER degrader 11 is promising for research of breast cancer brain metastasis .

HY-153023

PROTAC STAT3 degrader-2	PROTACs STAT	Cancer
PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC₅₀ of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research . PROTAC STAT3 degrader-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-176444B

(S)-CDK2 degrader 6	CDK Molecular Glues	Cancer
(S)-CDK2 degrader 6 (Compound 8) is the S-enantiomer of CDK2 degrader 6 (HY-176444). (S)-CDK2 degrader 6 is a selective CDK2 molecular glue degrader with a DC₅₀ of 166.7 nM in 24 h. (S)-CDK2 degrader 6 can be used for breast cancer research .

Cat. No.	Product Name

HY-L180

Mitophagy Compound Library

427 compounds

Mitochondrial autophagy refers to the selective encapsulation and degradation of damaged mitochondria by cells through the autophagy mechanism, thereby maintaining mitochondrial and cellular homeostasis. The concept of mitochondrial autophagy has received extensive attention since it was proposed. Current studies have shown that the mechanisms of mitochondrial autophagy can generally be divided into two categories: Ubiquitin-dependent pathways and Ub-independent pathways. In addition, mitochondrial autophagy is a research hotspot related to the pathogenesis of neurodegenerative diseases, cardiovascular diseases, cancer, metabolic diseases and other clinical diseases. Therefore, high-throughput screening based on mitochondrial autophagy can effectively screen out compounds that are closely related to the occurrence of diseases and analyze their mechanisms.

MCE can provide a library of 427 mitophagy compounds, which can be used for drug development and mechanism research in cancer, immunity, infection and other hot research fields.

Cat. No.	Product Name	Type

HY-N8332

Bile extract Ox bile extract	Biochemical Assay Reagents
Bile extract (Ox bile extract) is a complex mixture of substances, containing bile acids, cholesterol, and bilirubin. Bile extract has antimicrobial activity and can induce DNA damage and degrade viral and bacterial membranes. Bile extract can be used in bacterial culture media as a selective inhibitor for the isolation and identification of pathogens .

Cat. No.	Product Name	Target	Research Area

HY-P10331

KSL 128114	SDCBP	Cancer
KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .

HY-P5559

ND1-YL2	PROTACs	Cancer
ND1-YL2 is a PROTAC that selectively degrades SRC-1 via the N-degron pathway. ND1-YL2 significantly inhibits cancer invasion and migration in vitro and in vivo. ND1-YL2 can be used in cancer research .

HY-103294

R892	Endogenous Metabolite	Others
R892 is a selective and efficient bradyK_inin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .

HY-132604

Fazirsiran ARO-AAT	Small Interfering RNA (siRNA)	Metabolic Disease
Fazirsiran (ARO-AAT) is a second-generation RNAi agent. Fazirsiran consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.

HY-P2055

A-57696	Endogenous Metabolite	Endocrinology
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .

HY-P5377

Abz-HPGGPQ-EDDnp Cathepsin K substrate	Ser/Thr Protease	Others
Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)

Cat. No.	Product Name	Target	Research Area

HY-P991235

FS102 BMS-986186	EGFR Caspase	Cancer
FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a K_D value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer .

HY-P991243

MP-RM-1	EGFR PI3K Akt	Cancer
MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2419

Erythrodiol 1 Publications Verification	Triterpenes other families Canarium album (Lour.) Rauesch. Classification of Application Fields Terpenoids Source classification Metabolic Disease Plants Endogenous metabolite Burseraceae Disease Research Fields	Endogenous Metabolite
Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis .

HY-W010041

Scyllo-Inositol	Natural Products Source classification Endogenous metabolite	α-synuclein Amyloid-β
Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .

HY-B1247

Protoporphyrin IX 15+ Cited Publications	Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Other Diseases Endogenous metabolite Disease Research Fields	Endogenous Metabolite
Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .

HY-156193

PF-07208254	Cardiovascular Disease Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields	PDHK
PF-07208254 is a selective, orally active allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase (BDK) (IC₅₀=110 nM, K_i=54 nM, K_D=84 nM). PF-07208254 inhibits BDK-mediated BCKDH phosphorylation and enhances the catabolism of branched-chain amino acids (BCAAs) and branched-chain keto acids (BCKAs) by binding to the allosteric pocket of BDK, reducing BDK binding to BCKDH-E2 and promoting BDK degradation. PF-07208254 inhibits BDK activity in human skeletal muscle cells (IC₅₀=540 nM) and has activity to improve cardiac function and metabolism. PF-07208254 can be used in the study of cardiometabolic diseases (e.g., heart failure, type 2 diabetes) .

HY-B1247R

Protoporphyrin IX (Standard)	Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Source classification Endogenous metabolite	Reference Standards Endogenous Metabolite
Protoporphyrin IX (Standard) is the analytical standard of Protoporphyrin IX. This product is intended for research and analytical applications. Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .

HY-N0086R

N6-Methyladenosine (Standard) 6-Methyladenosine (Standard); N-Methyladenosine (Standard)	Natural Products Microorganisms Source classification Endogenous metabolite	Endogenous Metabolite Influenza Virus Reference Standards
N6-Methyladenosine (Standard) is the analytical standard of N6-Methyladenosine. This product is intended for research and analytical applications. N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities. In Vitro: N6-methyladenosine (m6A) is selectively recognized by the human YTH domain family 2 (YTHDF2) protein to regulate mRNA degradation. N6-methyladenosine (m6A), a prevalent internal modification in the messenger RNA of all eukaryotes, is post-transcriptionally installed by m6A methyltransferase (e.g., MT-A70) within the consensus sequence of G(m6A)C (70%) or A(m6A)C (30%). N6-methyladenosine (m6A)-containing RNAs are greatly enriched in the YTHDF-bound portion and diminished in the flow-through portion . N6-methyladenosine (m6A), the most abundant internal RNA modification, functions in diverse biological processes, including regulation of embryonic stem cell self-renewal and differentiation. N6-methyladenosine (m6A) is a large protein complex, consisting in part of methyltransferase-like 3 (METTL3) and methyltransferase-like 14 (METTL14) catalytic subunits .

HY-N2419R

Erythrodiol (Standard)	Triterpenes other families Canarium album (Lour.) Rauesch. Terpenoids Source classification Plants Endogenous metabolite Burseraceae	Reference Standards Endogenous Metabolite
Erythrodiol (Standard) is the analytical standard of Erythrodiol. This product is intended for research and analytical applications. Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis .

HY-W010041R

Scyllo-Inositol (Standard)	Natural Products Source classification Endogenous metabolite	α-synuclein Amyloid-β
Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .

HY-129200

Aspergillomarasmine A	Human Gut Microbiota Metabolites Microorganisms Source classification Endogenous metabolite	Endogenous Metabolite
Aspergillomarasmine A is a natural aminopolycarboxylic acid with potent inhibitory activity against class B metallo-β-lactamases (MBLs). Aspergillomarasmine A inactivates MBLs by removing a catalytic Zn2+ cofactor. Aspergillomarasmine A acts as a selective Zn2+ scavenger, promoting the dissociation of the metal cofactor, thereby indirectly inactivating NDM-1. Aspergillomarasmine A causes the loss of Zn2+ ions from the low-affinity binding site of NDM-1. The action of Aspergillomarasmine A results in the rapid degradation of Zn2+-deficient NDM-1, thereby enhancing its potency as a β-lactam enhancer. The mechanism of Aspergillomarasmine A has broad applicability among different Zn2+ chelators .

HY-W014394R

Vanillyl butyl ether (Standard)	Monophenols other families Source classification Phenols Plants	TRP Channel Reference Standards Parasite
Protoporphyrin IX (Standard) is the analytical standard of Protoporphyrin IX. This product is intended for research and analytical applications. Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .

Cat. No.	Product Name	Chemical Structure

HY-A0003S

Lenalidomide-d5

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 .

HY-13749AS

Sitagliptin-d4 phosphate

Sitagliptin-d₄ phosphate (MK-0431-d₄) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.

HY-19822S1

Elacestrant-d4-1
Elacestrant-d₄-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC₅₀s of 48 and 870 nM for ERα and ERβ, respectively .

HY-19822S2

Elacestrant-d10
Elacestrant-d₁₀ is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC₅₀s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER ⁺ breast cancer cell lines in vitro and in vivo .

HY-19822S3

Elacestrant-d6
Elacestrant-d₆ (RAD1901-d₆) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC₅₀ values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER ⁺ breast cancer cell lines both in vitro and in vivo.

HY-19822S

Elacestrant-d4
Elacestrant-d₄ (RAD1901-d₄) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC₅₀ values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER ⁺ breast cancer cell lines both in vitro and in vivo.

HY-13001S

Quizartinib-d8

Quizartinib-d₈ (AC220-d₈) is deuterium labeled Quizartinib. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a K_d of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC₅₀s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .

HY-A0003S2

Lenalidomide-13C5,15N

Lenalidomide- ¹³C₅, ¹⁵N is ¹⁵N and ¹³C labeled Lenalidomide (HY-A0003). 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-A0003S3

Lenalidomide-d4

Lenalidomide-d₄ (CC-5013-d₄) 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 .

HY-W707693

Scyllo-Inositol-d6

Scyllo-Inositol-d₆ is the deuterium labeled Scyllo-Inositol (HY-W010041). Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .

HY-13749S3

Sitagliptin-d6

Sitagliptin-d₆ (MK-0431-d₆) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.

HY-13749S2

Sitagliptin-d4

Sitagliptin-d₄ (MK-0431-d₄) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.

HY-13749S1

Sitagliptin-d4 hydrochloride

Sitagliptin-d₄ hydrochloride is the deuterium labeled Sitagliptin hydrochloride (HY-13749E). Sitagliptin hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.

Cat. No.	Product Name		Classification

HY-147943

PROTAC BTK Degrader-1		PROTAC Synthesis
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC₅₀ value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-147858

PROTAC EGFR degrader 7		PROTAC Synthesis Alkynes
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR ^L858R/T790M degrader, with a DC₅₀ of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC₅₀ of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-129602

SD-36 5+ Cited Publications		PROTAC Synthesis
SD-36 is a potent and efficacious STAT3 PROTAC degrader (K_d=~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 . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-69220

7-Octynoic acid		PROTAC Synthesis Alkynes
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 . 7-Octynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-153665

Deg-1		Azide
Deg-1 is a a bifunctional probe with a cleavage group and a covalent binding group. Deg-1 covalently binds to the target nucleic acid, and serves as click-degrader to cleave a nucleic acid molecule. Deg-1 has potential to selectively cleave target nucleic acids in cells . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.

HY-178925

PROTAC GPX4 degrader-5		Alkynes
PROTAC GPX4 degrader-5 is an efficient and highly selective GPX4 PROTAC degrader (DC₅₀ = 28 nM). PROTAC GPX4 degrader-5 can induce ferroptosis and has low toxicity to normal cells. PROTAC GPX4 degrader-5 can significantly increase ROS. PROTAC GPX4 degrader-5 exerts anti proliferative effects on various tumor cells. PROTAC GPX4 degrader-5 is commonly used in cancer research. (Pink: GPX4 Ligand (HY-179294); Blue: Hyt Hydrophobic group (HY-N2427); Black: Linker (HY-W047688))

HY-150251

SD-91 STAT3 degrader-2		PROTAC Synthesis
SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a K_i of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506) .

HY-139999

LCL-PEG3-N3		Azide
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 . LCL-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-139999A

LCL-PEG3-N3 hydrochloride		Azide
LCL-PEG3-N3 (hydrochloride) is a decoy oligonucleotide ligand for E3 ligase which can be used for developing chimeric molecules LCL-ER(dec), degrading the estrogen receptor . LCL-PEG3-N3 (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-169392

D5B		DBCO
D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC₅₀ of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity .

HY-107453

SirReal1-O-propargyl PROTAC Sirt2-binding moiety 1		Alkynes
SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC₅₀ of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2 . SirReal1-O-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-125843

Pomalidomide-PEG1-C2-N3 Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50		PROTAC Synthesis Azide
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 . Pomalidomide-PEG1-C2-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-108374

4-Azidobutylamine		Azide PROTAC Synthesis
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 . 4-Azidobutylamine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-130985

9-Decyn-1-ol		Alkynes PROTAC Synthesis
9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC₅₀s of 2.0 nM, 6.8 nM and 3.5 nM, respectively . 9-Decyn-1-ol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name		Classification

HY-132604A

Fazirsiran sodium ARO-AAT sodium		siRNAs siRNA drugs
Fazirsiran sodium is a second-generation RNAi agent. Fazirsiran sodium consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran sodium can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.

HY-159711

PPPDA-O16B		Cationic Lipids
PPPDA-O16B is a lipid containing disulfide bonds used for DNA delivery. PPPDA-O16B can encapsulate DNA plasmid, releasing DNA selectively via lipid degradation catalyzed by GSH .