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Linker optimization

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (4) Autophagy (1) Drug Derivative (1) Elastase (1) Epigenetic Reader Domain (1) FAP (1) FLT3 (4) Integrin (1) Isotope-Labeled Compounds (1) Ligands for Target Protein for PROTAC (4) PROTAC Linkers (2) PROTACs (1) Reference Standards (1)
By Research Areas:	Cancer (9)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: ADC Linker Target Protein Ligand-Linker Conjugates PROTAC-Linker Conjugates for PAC Drug-Linker Conjugates for ADC E3 Ligase Ligand-Linker Conjugates

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-124669

RTC-30	Drug Derivative	Cancer
RTC-30 is an optimized phenothiazine with anti-cancer potency. RTC-30 contains a hydroxylated linker (N) that confers increased oral bioavailability .

HY-W109760

FmocNH-PEG2-CH2CONH-PEG2-CH2COOH	PROTAC Linkers	Cancer
FmocNH-PEG2-CH2CONH-PEG2-CH2COOH is an optimized, extended PEG-like linker ^{[1] ^.}

HY-N8326

Maltononaose	Others	Others
Maltononaose is a linear oligosaccharide consisting of 9 glucose units linked by alpha-1, 4-glucoside bonds. Maltononaose is used as a substrate to study the subsites affinity of glucoamylase. Maltononaose can be used to determine the activity of amylase and to optimize the process of starch hydrolysis .

HY-13001

Quizartinib 40+ Cited Publications AC220; AC708	FLT3 Ligands for Target Protein for PROTAC Apoptosis	Cancer
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-14217

Quizartinib dihydrochloride 40+ Cited Publications AC220 dihydrochloride	FLT3 Apoptosis Ligands for Target Protein for PROTAC	Cancer
Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001). Quizartinib dihydrochloride 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 dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC₅₀s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis .

HY-114322A

cis-VZ185	PROTACs Epigenetic Reader Domain	Others
cis-VZ185 is a VHL-based PROTACs degrader with the activity of degrading BRD9 and BRD7. cis-VZ185 can be optimized from suboptimal compounds by optimizing the connection mode and linker, and has efficient, rapid and selective degradation of BRD9 and its homologous protein BRD7.

HY-W012935

Piperidine-4-carbaldehyde Piperidine-4-carboxaldehyde	PROTAC Linkers	Cancer
Piperidine-4-carbaldehyde (Piperidine-4-carboxaldehyde) is a PROTAC Linker. Piperidine-4-carbaldehyde can be used to optimize combined with the target protein affinity, thus improve the PROTAC the molecular degradation efficiency. Piperidine-4-carbaldehyde can be used in the CDK2 PROTACs (HY-161708) .

HY-164429

VIP236	Integrin Elastase	Cancer
VIP236 is a small-molecule-drug conjugates (SMDCs) consisting of an αvβ3 integrin binder linked to an optimized Camptothecin (HY-16560) topoisomerase I (TOP1) inhibitor payload. VIP236 exerts anticancer activity by targeting αvβ3 integrins, and it can release payload upon cleavage by neutrophil elastase in the tumor microenvironment .

HY-13001R

Quizartinib (Standard) AC220 (Standard); AC708 (Standard)	Reference Standards FLT3 Ligands for Target Protein for PROTAC Apoptosis Autophagy	Cancer
Quizartinib (Standard) is the analytical standard of Quizartinib. This product is intended for research and analytical applications. 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-13001S

Quizartinib-d8 AC220-d₈; AC708-d₈	Isotope-Labeled Compounds Ligands for Target Protein for PROTAC Apoptosis FLT3	Cancer
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-159771

FAP6-19	FAP	Cancer
FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a K_d of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as ¹⁷⁷Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with ¹¹¹In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.

Cat. No.	Product Name

HY-L918

Molecular Glue-like Compound Library	318 compounds
Targeted Protein Degradation (TPD) is a novel and promising approach to drug development. It shows great potential for targeting proteins traditionally considered "undruggable" due to the lack of enzymatic function and absence of binding sites by tagging them for degradation or recruiting natural degradation mechanisms. Molecular glues are a type of small-molecule degraders that primarily induce novel interactions between E3 ubiquitin ligases and target proteins, forming ternary complexes that lead to protein ubiquitination and subsequent proteasomal degradation. Compared with PROTACs, molecular glues generally have lower molecular weights, higher cell permeability, and better drug-like properties. Additionally, the design of molecular glues is relatively simple, without the requirements for complex linkers and ligand optimization. As a result, molecular glues have gradually emerged as a promising therapeutic approach for various diseases. Multiple types of molecular glues have been reported previously. Analysis of co-crystal complex structures reveals that CRBN-related molecular glues are more versatile. Therefore, MCE researchers select active molecules related to these targets as probes for artificial intelligence (AI) screening.Subsequently, molecular docking technology was used to verify whether the screened molecules retained the key pharmacophore features. Ultimately, we obtained 320 molecular glue analogs, and these compounds serve as powerful tools for the research of molecular glues.

Molecular Glue-like Compound Library

318 compounds

Targeted Protein Degradation (TPD) is a novel and promising approach to drug development. It shows great potential for targeting proteins traditionally considered "undruggable" due to the lack of enzymatic function and absence of binding sites by tagging them for degradation or recruiting natural degradation mechanisms.

Molecular glues are a type of small-molecule degraders that primarily induce novel interactions between E3 ubiquitin ligases and target proteins, forming ternary complexes that lead to protein ubiquitination and subsequent proteasomal degradation. Compared with PROTACs, molecular glues generally have lower molecular weights, higher cell permeability, and better drug-like properties. Additionally, the design of molecular glues is relatively simple, without the requirements for complex linkers and ligand optimization. As a result, molecular glues have gradually emerged as a promising therapeutic approach for various diseases.

Multiple types of molecular glues have been reported previously. Analysis of co-crystal complex structures reveals that CRBN-related molecular glues are more versatile. Therefore, MCE researchers select active molecules related to these targets as probes for artificial intelligence (AI) screening.Subsequently, molecular docking technology was used to verify whether the screened molecules retained the key pharmacophore features. Ultimately, we obtained 320 molecular glue analogs, and these compounds serve as powerful tools for the research of molecular glues.

Cat. No.	Product Name	Target	Research Area

HY-159771

FAP6-19	FAP	Cancer
FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a K_d of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as ¹⁷⁷Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with ¹¹¹In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N8326

Maltononaose	Polysaccharides Microorganisms Source classification Saccharides	Others
Maltononaose is a linear oligosaccharide consisting of 9 glucose units linked by alpha-1, 4-glucoside bonds. Maltononaose is used as a substrate to study the subsites affinity of glucoamylase. Maltononaose can be used to determine the activity of amylase and to optimize the process of starch hydrolysis .

Cat. No.	Product Name	Chemical Structure

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 .

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 .

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