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Results for "

Double degraders

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (3) Bcl-2 Family (1) Cyclic GMP-AMP Synthase (1) DNA/RNA Synthesis (2) Drug Intermediate (1) E1/E2/E3 Enzyme (1) Endonuclease (1) Environmental Pollutants (1) Herbicide (2) HIF/HIF Prolyl-Hydroxylase (2) HPPD (2) HSP (1) MDM-2/p53 (2) PARP (1) PD-1/PD-L1 (1) PROTACs (4) RAD51 (3) Reference Standards (2) Small Interfering RNA (siRNA) (2)
By Research Areas:	Cancer (11) Infection (1) Inflammation/Immunology (1)
Click Chemistry:	PROTAC Synthesis (1)
Oligonucleotides:	Guanosine (1) Nucleoside Analogs (1) siRNA drugs (2) siRNAs (2)

Inhibitors & Agonists

Screening Libraries

Click Chemistry

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P2773

Nuclease S1, Aspergillus oryzae	DNA/RNA Synthesis	Others
Nuclease S1, Aspergillus oryzae is a specific endonuclease that degrades single stranded DNA (ssDNA) and RNA. Nuclease S1 can also remove protruding single-strand ends from double-stranded DNA .

HY-114312

MD-224 5+ Cited Publications	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC₅₀ value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 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-103710

IBR2 5+ Cited Publications	RAD51 Apoptosis	Cancer
IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis .

HY-172208

PROTAC cGAS degrader-1	PROTACs Cyclic GMP-AMP Synthase	Inflammation/Immunology
PROTAC cGAS degrader-1 is a potent and selective cGAS PROTAC degrader, with DC₅₀ values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 induces proteasome-mediated degradation of cGAS, inhibits the cGAS signaling pathway, and attenuates double-stranded DNA-induced activation of cGAS in human and mouse cells. PROTAC cGAS degrader-1 is applicable to research related to ulcerative colitis .

HY-161410

WH244	PROTACs Apoptosis Bcl-2 Family	Cancer
WH244 is a second generation BCL-2 and BCL-xL dual depressant (PROTAC). The primary activity of WH244 is the specific degradation of BCL-2 and BCL-xL proteins (BCL-xL: DC₅₀=0.6 nM, BCL-2: DC₅₀=7.4 nM). WH244 promotes their ubiquitination and subsequent proteasome degradation by targeting these proteins, thereby restoring the cell's apoptosis pathway. WH244 has good antitumor activity. (Pink: BCL-2/BCL-xL ligand (HY-161415); Blue: E3 ligase ligand (HY-112078); Black: linker) .

HY-137910

Tembotrione	Environmental Pollutants HPPD Herbicide	Infection
Tembotrione is a herbicide belonging to the HPPD (dioxygenase) inhibitor class with crop selectivity. Tembotrione effectively controls a variety of weeds including broadleaf and gramineous species by disrupting carotenoid synthesis, which leads to chlorophyll degradation and leaf whitening. Mixing Tembotrione with isoxaflutole or adding surfactants optimizes its efficacy and reduces phytotoxicity, with no residual impact on subsequent cruciferous crops, thus helping to increase maize grain yield. The activity of Tembotrione decreases under drought conditions, and under specific conditions (such as double-dose treatment), it may cause reversible yellowing and even yield reduction in crops such as poppy .

HY-170844

MU147	Endonuclease	Cancer
MU147 is an MRE11 nuclease inhibitor and chemical probe with anticancer activity, which is lethal to Ehrlich ascites tumor cells both in vitro and in vivo. MU147 also eliminates the double-strand break repair mechanism dependent on the MRE11 nuclease activity without impairing the activation of ATM. MU147 also impairs the degradation of nascent strands of stalled replication FOX and selectively affects brca2-deficient cells .

HY-147426

Zifcasiran ADS-007; ARO HIF2	Small Interfering RNA (siRNA) HIF/HIF Prolyl-Hydroxylase	Cancer
Zifcasiran (ADS-007; ARO HIF2) is an siRNA synthetic double-stranded RNAi trigger. Zifcasiran sodium selectively target hypoxia-inducible factor-2α (HIF2α) interrupting downstream pro-oncogenic signaling in clear cell renal cell carcinoma (ccRCC). Zifcasiran sodium engages the cell's RNAi machinery to target HIF2α (EPAS1) mRNA for degradation, thereby reducing the amount of free HIF2α mRNA available for translation .

HY-146325

HSP90-IN-11	HSP	Cancer
HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .

HY-21286

N2-Isobutyryl-2'-O-methylguanosine	Drug Intermediate	Others
N2-Isobutyryl-2'-O-methylguanosine is a nucleic acid synthesis intermediate (e.g., used in antisense oligonucleotides, mRNA modification), for example, it is a key monomer for the synthesis of 2'-O-methyl oligoribonucleotides. N2-Isobutyryl-2'-O-methylguanosine enables the final product to form stable double strands with complementary RNA and is not easily degraded by nucleases. N2-Isobutyryl-2'-O-methylguanosine is mainly used in molecular biology research, and can be used to prepare RNA hybridization probes or participate in related biochemical research such as pre-mRNA splicing mechanisms .

HY-147426A

Zifcasiran sodium ADS-007 sodium; ARO HIF2 sodium	Small Interfering RNA (siRNA) HIF/HIF Prolyl-Hydroxylase	Cancer
Zifcasiran (ADS-007) sodium is an siRNA synthetic double-stranded RNAi trigger. Zifcasiran sodium selectively target hypoxia-inducible factor-2α (HIF2α) interrupting downstream pro-oncogenic signaling in clear cell renal cell carcinoma (ccRCC). Zifcasiran sodium engages the cell's RNAi machinery to target HIF2α (EPAS1) mRNA for degradation, thereby reducing the amount of free HIF2α mRNA available for translation .

HY-103710A

(R)-IBR2	RAD51	Cancer
(R)-IBR2 is the isomer of IBR2 (HY-103710). IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis .

HY-153200

MDM2/XIAP-IN-2	MDM-2/p53	Cancer
MDM2/XIAP-IN-2 is a dual inhibitor of *murine double* minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP*). MDM2/XIAP-IN-2 degrades* MDM2, and inhibits XIAP mRNA translation to inhibits cancer cells. Particularly, MDM2/XIAP-IN-2 inhibits acute lymphoblastic leukemia cell line EU-1 with an IC₅₀ value of 0.3 μM .

HY-137910R

Tembotrione (Standard)	Reference Standards Herbicide HPPD	Others
Tembotrione (Standard) is the analytical standard of Tembotrione. This product is intended for research and analytical applications. Tembotrione is a drug that may reduce the productivity of carrots. Tembotrione has the activity of reducing carrot stem mass. Tembotrione can be used to study the total productivity of carrot . Tembotrione is a herbicide belonging to the HPPD (dioxygenase) inhibitor class with crop selectivity. Tembotrione effectively controls a variety of weeds including broadleaf and gramineous species by disrupting carotenoid synthesis, which leads to chlorophyll degradation and leaf whitening. Mixing Tembotrione with isoxaflutole or adding surfactants optimizes its efficacy and reduces phytotoxicity, with no residual impact on subsequent cruciferous crops, thus helping to increase maize grain yield. The activity of Tembotrione decreases under drought conditions, and under specific conditions (such as double-dose treatment), it may cause reversible yellowing and even yield reduction in crops such as poppy .

HY-181967

PROTAC PARP1 degrader-5	PROTACs PARP DNA/RNA Synthesis PD-1/PD-L1	Cancer
PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC₅₀ of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma .

HY-103710R

IBR2 (Standard)	Reference Standards RAD51 Apoptosis	Cancer
IBR2 (Standard) is the analytical standard of IBR2 (HY-103710). This product is intended for research and analytical applications. IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis .

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library	174 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2). MCE carefully prepared a unique collection of 174 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

E3 Ligase Ligand Library

174 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.

Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).

MCE carefully prepared a unique collection of 174 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

Cat. No.	Product Name		Classification

HY-114312

MD-224 5+ Cited Publications		PROTAC Synthesis
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC₅₀ value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 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-147426

Zifcasiran ADS-007; ARO HIF2		siRNAs siRNA drugs
Zifcasiran (ADS-007; ARO HIF2) is an siRNA synthetic double-stranded RNAi trigger. Zifcasiran sodium selectively target hypoxia-inducible factor-2α (HIF2α) interrupting downstream pro-oncogenic signaling in clear cell renal cell carcinoma (ccRCC). Zifcasiran sodium engages the cell's RNAi machinery to target HIF2α (EPAS1) mRNA for degradation, thereby reducing the amount of free HIF2α mRNA available for translation .

HY-21286

N2-Isobutyryl-2'-O-methylguanosine		Nucleoside Analogs Guanosine
N2-Isobutyryl-2'-O-methylguanosine is a nucleic acid synthesis intermediate (e.g., used in antisense oligonucleotides, mRNA modification), for example, it is a key monomer for the synthesis of 2'-O-methyl oligoribonucleotides. N2-Isobutyryl-2'-O-methylguanosine enables the final product to form stable double strands with complementary RNA and is not easily degraded by nucleases. N2-Isobutyryl-2'-O-methylguanosine is mainly used in molecular biology research, and can be used to prepare RNA hybridization probes or participate in related biochemical research such as pre-mRNA splicing mechanisms .

HY-147426A

Zifcasiran sodium ADS-007 sodium; ARO HIF2 sodium		siRNAs siRNA drugs
Zifcasiran (ADS-007) sodium is an siRNA synthetic double-stranded RNAi trigger. Zifcasiran sodium selectively target hypoxia-inducible factor-2α (HIF2α) interrupting downstream pro-oncogenic signaling in clear cell renal cell carcinoma (ccRCC). Zifcasiran sodium engages the cell's RNAi machinery to target HIF2α (EPAS1) mRNA for degradation, thereby reducing the amount of free HIF2α mRNA available for translation .

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