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bifunctional molecule

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By Targets:	Antibiotic (1) Apoptosis (2) Aurora Kinase (1) Bacterial (1) Biochemical Assay Reagents (3) CXCR (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (4) Fluorescent Dye (1) HDAC (1) HIV (1) LYTACs (2) mAChR (1) MDM-2/p53 (1) Molecular Glues (2) mTOR (1) Phosphodiesterase (PDE) (1) Polo-like Kinase (PLK) (1) PROTACs (3) Reactive Oxygen Species (ROS) (1)
By Research Areas:	Cancer (12) Infection (1) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (1)
Click Chemistry:	Azide (2) Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Natural
Products

Click Chemistry

Targets Recommended: Repulsive guidance molecule ALCAM/CD166

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-D0967

Cy5-bifunctional dye	Fluorescent Dye	Others
Cy5-bifunctional dye is a Cy5 (HY-D0821) analog with two NHS esters. Cy5-bifunctional dye can be used to label the primary amines (R-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules .

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-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-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-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-159758

EcDHFR/FKBP12 F36V binder-1	Others	Neurological Disease Cancer
EcDHFR/FKBP12 F36V binder-1 (compound 1) is a bifunctional molecule that combines the Escherichia coli dihydrofolate reductase domain (EcDHFR) with the FKBP12 F36V domain .

HY-171561G

DOTAM-Maleimide triTFA	Biochemical Assay Reagents	Others
DOTAM-Maleimide triTFA (GMP) is DOTAM-Maleimide triTFA (HY-171561) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DOTAM-Maleimide triTFA is a bifunctional chelator .

HY-159004

Se-DOPE	Reactive Oxygen Species (ROS)	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-153665

Deg-1	Biochemical Assay Reagents	Others
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-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-132975

PrDiAzK	Bacterial	Others
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-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-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-138642

Vepdegestrant 3 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-170405

YB-3–17	PROTACs mTOR	Cancer
YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC₅₀=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC₅₀=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC₅₀ of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))

HY-173499

HLDA-212	Aurora Kinase Apoptosis	Cancer
HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI₅₀ of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies) .

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

HY-L222

PROTAC Linkers Library	0 compounds
Linkers play a necessary role in the physicochemical properties and biological activity of the bifunctional molecule. These linkers are not a simply connection of two functional modules together, but its design and nature directly affect the stability, activity, selectivity, pharmacokinetics, and ultimately the therapeutic efficacy of the entire molecule. The length of the linker determines the extent of interaction between the two ligands and thus the maximum activity of the PROTAC molecule. MCE has collected 0 PROTAC Linkers can be used for the design and synthesis of bifunctional molecules.

PROTAC Linkers Library

0 compounds

Linkers play a necessary role in the physicochemical properties and biological activity of the bifunctional molecule. These linkers are not a simply connection of two functional modules together, but its design and nature directly affect the stability, activity, selectivity, pharmacokinetics, and ultimately the therapeutic efficacy of the entire molecule. The length of the linker determines the extent of interaction between the two ligands and thus the maximum activity of the PROTAC molecule.

MCE has collected 0 PROTAC Linkers can be used for the design and synthesis of bifunctional molecules.

Cat. No.	Product Name	Type

HY-D0967

Cy5-bifunctional dye	Dyes
Cy5-bifunctional dye is a Cy5 (HY-D0821) analog with two NHS esters. Cy5-bifunctional dye can be used to label the primary amines (R-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules .

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 .

HY-171561G

DOTAM-Maleimide triTFA (GMP)	Fluorescent Dye
DOTAM-Maleimide triTFA (GMP) is DOTAM-Maleimide triTFA (HY-171561) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DOTAM-Maleimide triTFA is a bifunctional chelator .

Cat. No.	Product Name	Type

HY-171561G

DOTAM-Maleimide triTFA (GMP)	Biochemical Assay Reagents
DOTAM-Maleimide triTFA (GMP) is DOTAM-Maleimide triTFA (HY-171561) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DOTAM-Maleimide triTFA is a bifunctional chelator .

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	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-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 .

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.

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bifunctional molecule

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

NaturalProducts

Click Chemistry

Natural
Products