Structure-activity relationship (SAR)

By Targets:	Apelin Receptor (APJ) (1) Apoptosis (1) Casein Kinase (1) CDK (1) Cuproptosis (1) DNA/RNA Synthesis (1) Drug Intermediate (3) Keap1-Nrf2 (1) Phosphoglycerate Kinase (PGK) (1) TRP Channel (1)
By Research Areas:	Cancer (7) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W007614

3-Fluoro-4-methoxybenzaldehyde 3-Fluoro-para-anisaldehyde	Drug Intermediate	Cancer
3-Fluoro-4-methoxybenzaldehyde (3-Fluoro-para-anisaldehyde) is a drug intermediate that can be used to synthesize the fluorinated derivative of Combretastatin A-4 (HY-N2146), which has anti-cancer activity.

HY-75577

4-Amino-3-methoxybenzoic acid	Drug Intermediate	Cancer
4-Amino-3-methoxybenzoic acid is a drug intermediate that can be used to construct benzothiazole compounds with anti-breast cancer activity .

HY-40181

1-Boc-homopiperazine	Drug Intermediate	Infection
1-Boc-homopiperazine is a drug intermediate that can be used for the synthesis of bacterial FtsZ inhibitors .

HY-157928

Keap1-Nrf2-IN-18	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (K_D = 0.0029 μM) .

HY-178236

TRPM5 agonist-1	TRP Channel	Metabolic Disease
TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC₅₀ of 8.1. TRPM5 agonist-1 shows excellent selectivity (> 100-fold) versus related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4). TRPM5 agonist-1 exhibits locally acting stimulatory effect on gastrointestinal transit in mice. TRPM5 agonist-1 can be used for research on promoting gastric motility .

HY-178112

CDK2-IN-47	CDK Apoptosis	Cancer
CDK2-IN-47 is a potent CDK2 inhibitor with an IC₅₀ of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer .

HY-178991

WRN-IN-21	DNA/RNA Synthesis	Cancer
WRN-IN-21 (Compound 11b) is a WRN helicase inhibitor with pIC₅₀ values for WRN and BLM helicases of 3.6 and 5.4 respectively. WRN-IN-21 can be used for the study of MSI-related cancers .

HY-178989

PGK1-IN-2	Phosphoglycerate Kinase (PGK) Cuproptosis	Cancer
PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC₅₀ of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma .

HY-123853

CAM4066	Casein Kinase	Cancer
CAM4066 is a potent CK2α inhibitor, with an IC₅₀ value of 300 nM. CAM4066 exhibits high selectivity, with IC₅₀ values of 22.35, 43.55, and > 50 μM for HIPK3, DAPK3, and CLK2, respectively. CAM4066 shows no cell activity. CAM4066 can be used for the development of highly potent CK2 inhibitors .

HY-175818

APJ antagonist-1	Apelin Receptor (APJ)	Cancer
APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC₅₀ of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis .

Cat. No.	Product Name

HY-L927

10K Golden Scaffold Library	10000 compounds
Designed to maximize efficiency in hit discovery and optimization, this compound library is built on a foundation of diverse Bemis-Murcko scaffolds, with each scaffold is represented by two specifically derived molecules. This strategy ensures broad chemical space through scaffold diversity while enabling preliminary functional group exploration. This approach provides early structure-activity relationship (SAR) insights for every scaffold, making it a valuable tool for accelerating drug discovery.

10K Golden Scaffold Library

10000 compounds

Designed to maximize efficiency in hit discovery and optimization, this compound library is built on a foundation of diverse Bemis-Murcko scaffolds, with each scaffold is represented by two specifically derived molecules. This strategy ensures broad chemical space through scaffold diversity while enabling preliminary functional group exploration. This approach provides early structure-activity relationship (SAR) insights for every scaffold, making it a valuable tool for accelerating drug discovery.

Cat. No.	Product Name	Type

HY-W007614

3-Fluoro-4-methoxybenzaldehyde 3-Fluoro-para-anisaldehyde	Biochemical Assay Reagents
3-Fluoro-4-methoxybenzaldehyde (3-Fluoro-para-anisaldehyde) is a drug intermediate that can be used to synthesize the fluorinated derivative of Combretastatin A-4 (HY-N2146), which has anti-cancer activity.

HY-75577

4-Amino-3-methoxybenzoic acid	Biochemical Assay Reagents
4-Amino-3-methoxybenzoic acid is a drug intermediate that can be used to construct benzothiazole compounds with anti-breast cancer activity .

HY-40181

1-Boc-homopiperazine	Biochemical Assay Reagents
1-Boc-homopiperazine is a drug intermediate that can be used for the synthesis of bacterial FtsZ inhibitors .

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
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Screening Libraries

Biochemical Assay Reagents

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