therapeutics

By Targets:	Androgen Receptor (1) Bacterial (1) Caspase (1) DNA Methyltransferase (2) DNA Stain (3) Epigenetic Reader Domain (1) HIF/HIF Prolyl-Hydroxylase (1) Liposome (5) Nucleoside Antimetabolite/Analog (1) PI3K (1) SARS-CoV (1) TET Protein (2)
By Research Areas:	Cancer (10) Cardiovascular Disease (3) Endocrinology (1) Infection (3) Metabolic Disease (3) Neurological Disease (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12281

FPH2 BRD-9424	Others	Metabolic Disease Cancer
FPH2 induces of functional proliferation of primary human hepatocytes and may lead to the development of new therapeutics for liver diseases.

HY-114243

DpC

Others Cancer

DpC is an anti-tumor agent. DpC inhibits cancer cell proliferation (IC₅₀: 0.007-0.096 渭M). DpC synergizes with multiple anti-cancer therapeutics .

DpC	Others	Cancer
DpC is an anti-tumor agent. DpC inhibits cancer cell proliferation (IC₅₀: 0.007-0.096 渭M). DpC synergizes with multiple anti-cancer therapeutics .

HY-D1408

DMTr-4'-Me-U-CED-TBDMS phosphoramidite DMTr-4'-Methyluridine-CED-TBDMS phosphoramidite	DNA Stain	Cardiovascular Disease
DMTr-4'-Me-U-CED-TBDMS phosphoramidite (DMTr-4'-Methyluridine-CED-TBDMS phosphoramidite), a dye reagent for oligonucleotide labeling, can be used for the research of applications in RNA therapeutics, RNA aptamers, and ribozymes for elucidating RNA structure. DMTr-4'-Me-U-CED-TBDMS phosphoramidite represents a probe with wide utility for elucidation of RNA structure .

HY-D1409

DMTr-4'-F-U-CED-TBDMS phosphoramidite DMTr-4'-F-uridine-CED-TBDMS phosphoramidite	DNA Stain	Cardiovascular Disease
DMTr-4'-F-U-CED-TBDMS phosphoramidite (DMTr-4'-F-uridine-CED-TBDMS phosphoramidite), a dye reagent for oligonucleotide labeling, can be used for the research of applications in RNA therapeutics, RNA aptamers, and ribozymes for elucidating RNA structure. DMTr-4'-F-U-CED-TBDMS phosphoramidite represents a probe with wide utility for elucidation of RNA structure .

HY-145797

L343

Liposome Others

L343 is an ionizable cationic lipidoid and can be used to synthetic liposomes for systemic delivery of RNAi therapeutics.

L343	Liposome	Others
L343 is an ionizable cationic lipidoid and can be used to synthetic liposomes for systemic delivery of RNAi therapeutics.

HY-W441002

DSPE-succinic acid	Liposome	Others
DSPE-succinic acid is a phophalipid capped with a carboxylic acid moiety. The carboxylic acid moiety is reactive with amine to from a stable amide linkage. DSPE-succinic acid can be used to prepare nanoparticles or liposomes for agent nanocarrier to deliver therapeutics .

HY-134541

SM-102 5+ Cited Publications	Liposome	Infection
SM-102 is an amino cationic lipid useful in the formation of lipid nanoparticles (LNPs). SM-102 has higher transfection efficiency. SM-102 plays an important role in the effectiveness of lipid nanoparticles (LNPs) in delivering mRNA therapeutics and vaccines .

HY-109050

Alobresib 1 Publications Verification GS-5829	Epigenetic Reader Domain	Cancer
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research .

HY-136304

NHS-PEG1-SS-PEG1-NHS	Liposome	Cardiovascular Disease Metabolic Disease Cancer
NHS-PEG1-SS-PEG1-NHS is a reversible linker for biomacromolecule link with active small molecule. NHS-PEG1-SS-PEG1-NHS can be used in proteins liposomes or nanoparticles .

HY-111558A

Bobcat339 hydrochloride Maximum Cited Publications 14 Publications Verification	DNA Methyltransferase TET Protein	Cancer
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC₅₀s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription .

HY-111558

Bobcat339 Maximum Cited Publications 14 Publications Verification	DNA Methyltransferase TET Protein	Cancer
Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC₅₀s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription .

HY-139970

VPC-13789	Androgen Receptor	Endocrinology Cancer
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC₅₀=0.19 μM) .

HY-D1411

DMTr-4'-CF3-5-Me-U-CED phosphoramidite DMTr-4'-CF3-5-Methyluridine-CED phosphoramidite	DNA Stain	Others
DMTr-4'-CF3-5-Me-U-CED phosphoramidite (DMTr-4'-CF3-5-Methyluridine-CED phosphoramidite), the modified oligodeoxynucleotide (ODN), is a dye reagent for oligonucleotide labeling, can be used for the research of applications in RNA research .

HY-156168

M190S	Caspase	Cancer
M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability .

HY-157252

CL4F8-6	Liposome	Cancer
CL4F8-6 is an ionizable cationic lipid with a pK_a of 6.14. CL4F8-6 can be used in lipid nanoparticles (LNPs)-based mRNA therapeutics. CL4F8-6 LNPs carrying Cas9 mRNA and sgRNA could induce CRISPR-mediated gene knockdown in mice .

HY-157339

MMT-2'-O-Methyl adenosine (n-bz) CED phosphoramidite	Nucleoside Antimetabolite/Analog	Others
MMT-2'-O-Methyl adenosine (n-bz) CED phosphoramidite (compound 1) is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies .

HY-N0401A

(Z)-Ligustilide 2 Publications Verification	Bacterial	Infection Metabolic Disease
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .

HY-155280

SARS-CoV-2-IN-60	SARS-CoV	Infection
SARS-CoV-2-IN-60 (compound 5a) is an S-adenosylmethionine (SAM)-competitive and irreversible SARS-CoV-2 nsp16-nsp10 methyltransferase activity inhibitor with an IC₅₀ of 9 μM and a K_i of 26 μM. SARS-CoV-2-IN-60 can specifically occupy a newly identified pocket adjacent to the SAM-binding site on nsp16. SARS-CoV-2-IN-60 has the potential for pan-coronavirus therapeutics .

HY-155730

PI3K-IN-41	PI3K	Cancer
PI3K-IN-41 (compound 2) is a photocaged compound, as well as a photocaged PI3K inhibitor (IC₅₀=18.92 nM) with anticancer properties. PI3K-IN-41 has potential to be used in precisely controlled cancer therapeutics. PI3K-IN-41 exhibits potent PI3K ihibition upon UV light irradiation, and enhances antitumor effect .

HY-124875

Arylsulfonamide 64B HIF inhibitor 64B	HIF/HIF Prolyl-Hydroxylase	Neurological Disease
Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model .

Cat. No.	Product Name

HY-L110

Cyclic Peptide Library	84 compounds
Cyclic peptides are polypeptide chains taking cyclic ring structure, which exhibit diverse biological activities, such as antibacterial activity, immunosuppressive activity and anti-tumor activity. Cyclic peptides, with the features of good binding affinity, target selectivity and low toxicity, show great success as therapeutics. Multiple cyclic peptides are currently in clinical use, for examples, gramicidin and tyrocidine with bactericidal activity, cyclosporin A with immunosuppressive activity, and vancomycin with antibacterial activity. Furthermore, cyclic peptides usually have the sufficient size and a balanced conformational flexibility/rigidity for binding to flat protein-protein interaction (PPI) interfaces, which have potential to develop PPI drugs. MCE offers a unique collection of 84 cyclic peptides, all of which have good bioactivities. MCE Cyclic Peptide Library is a powerful tool for drug discovery and PPI inhibitor screening.

Cyclic Peptide Library

84 compounds

Cyclic peptides are polypeptide chains taking cyclic ring structure, which exhibit diverse biological activities, such as antibacterial activity, immunosuppressive activity and anti-tumor activity. Cyclic peptides, with the features of good binding affinity, target selectivity and low toxicity, show great success as therapeutics. Multiple cyclic peptides are currently in clinical use, for examples, gramicidin and tyrocidine with bactericidal activity, cyclosporin A with immunosuppressive activity, and vancomycin with antibacterial activity. Furthermore, cyclic peptides usually have the sufficient size and a balanced conformational flexibility/rigidity for binding to flat protein-protein interaction (PPI) interfaces, which have potential to develop PPI drugs.

MCE offers a unique collection of 84 cyclic peptides, all of which have good bioactivities. MCE Cyclic Peptide Library is a powerful tool for drug discovery and PPI inhibitor screening.

HY-L036

Covalent Screening Library	1670 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery. MCE covalent inhibitor library contains 1670 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

Covalent Screening Library

1670 compounds

Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.

MCE covalent inhibitor library contains 1670 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

HY-L036P

Covalent Screening Library Plus	2988 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery. MCE covalent inhibitor library contains 2988 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc. MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

Covalent Screening Library Plus

2988 compounds

Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.

MCE covalent inhibitor library contains 2988 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

Cat. No.	Product Name	Type

HY-D1408

DMTr-4'-Me-U-CED-TBDMS phosphoramidite DMTr-4'-Methyluridine-CED-TBDMS phosphoramidite	Oligonucleotide Labeling
DMTr-4'-Me-U-CED-TBDMS phosphoramidite (DMTr-4'-Methyluridine-CED-TBDMS phosphoramidite), a dye reagent for oligonucleotide labeling, can be used for the research of applications in RNA therapeutics, RNA aptamers, and ribozymes for elucidating RNA structure. DMTr-4'-Me-U-CED-TBDMS phosphoramidite represents a probe with wide utility for elucidation of RNA structure .

HY-D1409

DMTr-4'-F-U-CED-TBDMS phosphoramidite DMTr-4'-F-uridine-CED-TBDMS phosphoramidite	Oligonucleotide Labeling
DMTr-4'-F-U-CED-TBDMS phosphoramidite (DMTr-4'-F-uridine-CED-TBDMS phosphoramidite), a dye reagent for oligonucleotide labeling, can be used for the research of applications in RNA therapeutics, RNA aptamers, and ribozymes for elucidating RNA structure. DMTr-4'-F-U-CED-TBDMS phosphoramidite represents a probe with wide utility for elucidation of RNA structure .

Cat. No.	Product Name	Type

HY-134541

SM-102 5+ Cited Publications	Drug Delivery
SM-102 is an amino cationic lipid useful in the formation of lipid nanoparticles (LNPs). SM-102 has higher transfection efficiency. SM-102 plays an important role in the effectiveness of lipid nanoparticles (LNPs) in delivering mRNA therapeutics and vaccines .

HY-136304

NHS-PEG1-SS-PEG1-NHS	Drug Delivery
NHS-PEG1-SS-PEG1-NHS is a reversible linker for biomacromolecule link with active small molecule. NHS-PEG1-SS-PEG1-NHS can be used in proteins liposomes or nanoparticles .

HY-145797

L343

Drug Delivery

L343 is an ionizable cationic lipidoid and can be used to synthetic liposomes for systemic delivery of RNAi therapeutics.

L343	Drug Delivery
L343 is an ionizable cationic lipidoid and can be used to synthetic liposomes for systemic delivery of RNAi therapeutics.

HY-W441002

DSPE-succinic acid	Drug Delivery
DSPE-succinic acid is a phophalipid capped with a carboxylic acid moiety. The carboxylic acid moiety is reactive with amine to from a stable amide linkage. DSPE-succinic acid can be used to prepare nanoparticles or liposomes for agent nanocarrier to deliver therapeutics .

HY-157252

CL4F8-6	Drug Delivery
CL4F8-6 is an ionizable cationic lipid with a pK_a of 6.14. CL4F8-6 can be used in lipid nanoparticles (LNPs)-based mRNA therapeutics. CL4F8-6 LNPs carrying Cas9 mRNA and sgRNA could induce CRISPR-mediated gene knockdown in mice .

Cat. No.	Product Name	Target	Research Area

HY-P2342

Angiopep-Bim BH3 hydrochloride	Peptides	Neurological Disease
Angiopep-Bim BH3 hydrochloride, a BBB penetrated peptode, could be used to investigate the permeability of CNS therapeutics .

HY-P5415

DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS	Peptides	Others
DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is a biological active peptide. (DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is also called HIV protease substrate I in some literature. It is widely used for the continuous assay for HIV protease activity. The 11-kD protease (PR) encoded by the human immunodeficiency virus 1 (HIV-1) is essential for the correct processing of viral polyproteins and the maturation of infectious virus, and is therefore a target for the design of selective acquired immunodeficiency syndrome (AIDS) therapeutics. The FRET-based fluorogenic substrate is derived from a natural processing site for HIV-1 PR. Incubation of recombinant HIV-1 PR with the fluorogenic substrate resulted in specific cleavage at the Tyr-Pro bond and a time-dependent increase in fluorescence intensity that is linearly related to the extent of substrate hydrolysis. The fluorescence quantum yields of the HIV-1 PR substrate in the FRET assay increased by 40.0- and 34.4-fold, respectively, per mole of substrate cleaved. Because of its simplicity and precision in the determination of reaction rates required for kinetic analysis, this substrate offers many advantages over the commonly used HPLC or electrophoresis-based assays for peptide substrate hydrolysis by retroviral PRs. Abs/Em = 340nm/490nm.)

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0401A

(Z)-Ligustilide 2 Publications Verification	Structural Classification Natural Products Classification of Application Fields Source classification Metabolic Disease Dicerothamnus rhinocerotis Plants Umbelliferae Disease Research Fields	Bacterial
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Natural
Products