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bifunctional molecule

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By Targets:	Antibiotic (1) Apoptosis (1) Biochemical Assay Reagents (1) CXCR (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (4) HDAC (1) HIV (1) LYTACs (2) mAChR (1) MDM-2/p53 (1) Molecular Glues (2) Phosphodiesterase (PDE) (1) Polo-like Kinase (PLK) (1) PROTACs (2) Reactive Oxygen Species (1)
By Research Areas:	Cancer (9) Infection (1) Inflammation/Immunology (2) Metabolic Disease (1)
Click Chemistry:	Azide (2) Alkynes (1)

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Natural
Products

Click Chemistry

Targets Recommended: ALCAM/CD166

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-D2280

Estrogen receptor β/HDAC probe 1	HDAC Estrogen Receptor/ERR	Others
Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC .

HY-142881

D-MoDE-A (1)	LYTACs	Others
D-MoDE-A (1) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).

HY-142885

M-MoDE-A (2)	LYTACs	Others
M-MoDE-A (2) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).

HY-163811

BRD9 Degrader-4	Molecular Glues Epigenetic Reader Domain	Cancer
BRD9 Degrader-4 (BRD9c), a bifunctional molecular glue, is a potent BRD9 degrader with a DC₅₀ of ≤25 nM. BRD9 Degrader-4 has anti-cancer effects .

HY-163812

ER degrader 9	Molecular Glues Estrogen Receptor/ERR	Cancer
ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC₅₀ of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .

HY-159004

Se-DOPE	Reactive Oxygen Species	Metabolic Disease Inflammation/Immunology
Se-DOPE is a phospholipid molecule with selenium. Se-DOPE can be used to synthesize the bifunctional Janus liposozyme. Se-DOPE promotes the production of ROS with induction of lights, scavenges the ROS with the presence of glutathione. Se-DOPE regulates redox and immune homeostasis in infected diabetic wounds .

HY-W088413A

DOTA-amide dihydrate	Biochemical Assay Reagents	Cancer
DOTA-amide (dihydrate) is a Bifunctional Chelators (BFCs). DOTA-amide (dihydrate) binds to the Affibody molecule ZHER2:S1. Its complex binds specifically to HER2 and can be used to detect bone metastases, which are common in prostate cancer .

HY-155819

M3/PDE4 modulator-1	mAChR Phosphodiesterase (PDE)	Inflammation/Immunology
M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model .

HY-149558

CXCR4-IN-2	Apoptosis CXCR	Cancer
CXCR4-IN-2 (compound A1) is a bifunctional fluorinated small molecule that is a potent CXCR4 inhibitor with anticancer activity. CXCR4-IN-2 has cytotoxic (IC₅₀: 60 μg/mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. CXCR4-IN-2 induces cell arrest in the G2/M phase and induces apoptosis .

HY-130050

Luzopeptin A BBM-928 A	Antibiotic HIV	Infection Cancer
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC₅₀s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively .

HY-138642

Vepdegestrant 2 Publications Verification ARV-471	PROTACs Estrogen Receptor/ERR	Cancer
Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against 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 about 2 nM .

HY-138642A

(Rac)-Vepdegestrant (Rac)-ARV-471	Estrogen Receptor/ERR PROTACs	Cancer
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against 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 about 2 nM .

HY-159493

BI2536-PEG2-Halo	Polo-like Kinase (PLK)	Cancer
BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC₅₀=23 nM), exhibits selective toxicity against p53 mutant cancer cells .

HY-158685

RG7112D	MDM-2/p53	Cancer
RG7112D is a potent MDM2 inhibitor with IC₅₀s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC₅₀=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels .

Cat. No.	Product Name	Type

HY-D2280

Estrogen receptor β/HDAC probe 1	Fluorescent Dyes/Probes
Estrogen receptor β/HDAC probe 1 (compound P1) is a near-infrared fluorescent probe that dual-targets the estrogen receptor (Estrogen Receptor/ERR) β/histone deacetylase HDAC .

Cat. No.	Product Name	Type

HY-W088413A

DOTA-amide dihydrate	Chelators
DOTA-amide (dihydrate) is a Bifunctional Chelators (BFCs). DOTA-amide (dihydrate) binds to the Affibody molecule ZHER2:S1. Its complex binds specifically to HER2 and can be used to detect bone metastases, which are common in prostate cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-130050

Luzopeptin A BBM-928 A	Structural Classification Microorganisms Antibiotics Source classification	Antibiotic HIV
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC₅₀s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively .

Cat. No.	Product Name		Classification

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-132975

PrDiAzK		Alkynes
PrDiAzK is a bifunctional amino acid. PrDiAzK can be site-selectively incorporated into proteins in both bacterial and mammalian cell culture. PrDiAzK can be used for proteome-wide incorporation via stochastic orthogonal recoding of translation (SORT) . PrDiAzK 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-159493

BI2536-PEG2-Halo		Azide
BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC₅₀=23 nM), exhibits selective toxicity against p53 mutant cancer cells .

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bifunctional molecule

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

NaturalProducts

Click Chemistry

Natural
Products