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Results for "

target site resistance

" in MedChemExpress (MCE) Product Catalog:

標的別:	AAK1 (1) Acetolactate Synthase (ALS) (1) CDK (1) Cyclin G-associated Kinase (GAK) (1) Cytochrome P450 (1) Endogenous Metabolite (2) Environmental Pollutants (1) Glutathione S-transferase (1) Herbicide (1) LIM Kinase (LIMK) (1) Microtubule/Tubulin (1) PROTACs (1) Reactive Oxygen Species (ROS) (1) Reference Standards (1) Salt-inducible Kinase (SIK) (1) SHP2 (1) SnRK (1) SOD (1) Wee1 (1)
研究分野別:	Cancer (2) Metabolic Disease (2)
クリックケミストリー:	Alkynes (1)

阻害剤およびアゴニスト

スクリーニングライブラリ

天然物

クリックケミストリー

Targets Recommended: BCRP BMI1 P-glycoprotein

製品番号	製品名	Target	研究分野	構造式

HY-136426

Trifludimoxazin	Environmental Pollutants Reactive Oxygen Species (ROS) Herbicide	Others
Trifludimoxazin is a click chemistry reagent, a protoporphyrinogen oxidase (PPO) inhibitor and herbicide. Trifludimoxazin inhibits PPO, accumulates reactive oxygen species, damages cell membranes, and thereby causes weed death. Trifludimoxazin exhibits high-efficiency activity in controlling broadleaf weeds and grassy weeds .

HY-113138

3-Methyluridine 1 Publications Verification N3-Methyluridine	Endogenous Metabolite	Metabolic Disease
3-Methyluridine (m ³U; N3-Methyluridine) is a methylated nucleotide present in ribosomal RNA (rRNA), mainly targeting specific base sites of RNA molecules such as 23S rRNA. 3-Methyluridine can introduce a methyl group at the N3 position of uracil, affecting the secondary structure stability and base pairing ability of RNA, and regulating ribosome function. For example, it affects ribosomal subunit binding and tRNA interaction. 3-Methyluridine is often used as a key raw material for the synthesis of modified nucleotides, and is used to construct RNA oligonucleotides containing methylation modifications to study the effects of RNA methylation on gene expression and drug resistance .

HY-148062

RSS0680	PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK	Others
RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC with protein kinase degradation activity (Pink: FLT3-IN-17 (HY-148070); Black: Linker (HY-W041970); Blue: E3 ligase Ligand (HY-112078)). RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].

HY-121524

DJ101	Microtubule/Tubulin	Cancer
DJ101 is a potent and metabolically stable tubulin inhibitor. DJ101 targets the colchicine binding site and overcomes taxane resistance. DJ101 also inhibits melanoma tumor growth and lung metastasis. DJ101 can be used for prostate cancer research .

HY-170920

Herbicide safener-4	Cytochrome P450 SOD Glutathione S-transferase Acetolactate Synthase (ALS)	Others
Herbicide safener-4 (Compound I-15) is a Herbicide safener, improving the herbicide resistance of crops without reducing the herbicidal effect on targeted weed species. Herbicide safener-4 competitively binds to the ALS active site with Mesosulfuron-methyl (HY-126987). Herbicide safener-4 enhances GSH (HY-D0187), GST, CYP450, POD, SOD and ALS activity in plants .

HY-115527

SHP244	SHP2	Cancer
SHP244 is a conformational inhibitor targeting the "latch allosteric site" (site 2) of the SHP2 protein with an IC₅₀ value for SHP2 ^WT of 60 μM. SHP244 has no significant effect on the level of p-ERK alone. SHP244 combined with RMC-4550 (HY-116009) ("tunnel site" site 1 inhibitor) can reduce p-ERK and inhibit the rebound of p-ERK, thereby reducing drug resistance. SHP244 can be used to study drug resistance in FGFR-driven cancers .

HY-113138R

3-Methyluridine (Standard) N3-Methyluridine (Standard)	Endogenous Metabolite Reference Standards	Metabolic Disease
3-Methyluridine (Standard) is the analytical standard of 3-Methyluridine. This product is intended for research and analytical applications. 3-Methyluridine (m3U; N3-Methyluridine) is a methylated nucleotide present in ribosomal RNA (rRNA), mainly targeting specific base sites of RNA molecules such as 23S rRNA. 3-Methyluridine can introduce a methyl group at the N3 position of uracil, affecting the secondary structure stability and base pairing ability of RNA, and regulating ribosome function. For example, it affects ribosomal subunit binding and tRNA interaction. 3-Methyluridine is often used as a key raw material for the synthesis of modified nucleotides, and is used to construct RNA oligonucleotides containing methylation modifications to study the effects of RNA methylation on gene expression and drug resistance .

製品番号	製品名

HY-LD004

DEL Covalent Library	14 million compounds
DEL technology enables the simultaneous screening of millions or billions of compounds in a single tube by covalently linking each small molecule with a unique DNA sequence. Traditional DEL screening primarily focuses on identifying non-covalent binding molecules, where interactions with the target are reversible. In contrast, DNA‑encoded covalent library is an ultra‑high‑throughput screening library developed on the basis of conventional DNA‑encoded library technology. It incorporates controllable electrophilic covalent warheads capable of forming irreversible covalent bonds with amino acid residues at the active sites of target proteins, including Cys, Lys, Ser, Tyr, and others. This covalent binding enhances binding affinity, prolongs residence time at the target site, and has the potential to overcome challenges associated with traditional non-covalent inhibitors, such as drug resistance or off-target effects. Each compound in the library contains both a binding domain and an electrophilic warhead. It first recognizes and binds to the target through non covalent interactions, and then forms a stable covalent bond with key amino acid residues to achieve irreversible inhibition. This library is specifically designed for the discovery of potent, long lasting, and highly selective covalent inhibitors, particularly for undruggable targets such as kinases, GPCRs, proteases, and mutant oncoproteins. Each molecule is uniquely labeled with a DNA barcode for molecular identification and sequencing decoding. This library is an advanced and highly diverse collection, consists of 35 independent sub-libraries with a total scaleof 14 million compounds, It incorporates over 14 experimentally validated covalent warheads capable of targeting cysteine, lysine, arginine, aspartic acid and glutamic acid. This library is constructed with diverse drug like core scaffolds and integrated controllable covalent warheads, it features structural diversity, reaction spec

DEL Covalent Library

14 million compounds

DEL technology enables the simultaneous screening of millions or billions of compounds in a single tube by covalently linking each small molecule with a unique DNA sequence. Traditional DEL screening primarily focuses on identifying non-covalent binding molecules, where interactions with the target are reversible. In contrast, DNA‑encoded covalent library is an ultra‑high‑throughput screening library developed on the basis of conventional DNA‑encoded library technology. It incorporates controllable electrophilic covalent warheads capable of forming irreversible covalent bonds with amino acid residues at the active sites of target proteins, including Cys, Lys, Ser, Tyr, and others. This covalent binding enhances binding affinity, prolongs residence time at the target site, and has the potential to overcome challenges associated with traditional non-covalent inhibitors, such as drug resistance or off-target effects.

Each compound in the library contains both a binding domain and an electrophilic warhead. It first recognizes and binds to the target through non covalent interactions, and then forms a stable covalent bond with key amino acid residues to achieve irreversible inhibition. This library is specifically designed for the discovery of potent, long lasting, and highly selective covalent inhibitors, particularly for undruggable targets such as kinases, GPCRs, proteases, and mutant oncoproteins. Each molecule is uniquely labeled with a DNA barcode for molecular identification and sequencing decoding.

This library is an advanced and highly diverse collection, consists of 35 independent sub-libraries with a total scaleof 14 million compounds, It incorporates over 14 experimentally validated covalent warheads capable of targeting cysteine, lysine, arginine, aspartic acid and glutamic acid. This library is constructed with diverse drug like core scaffolds and integrated controllable covalent warheads, it features structural diversity, reaction spec

HY-L941

Allosteric Modulator Lead‑like Compound Library	4315 compounds
Owing to the high conservation of orthosteric sites, conventional orthosteric drugs frequently suffer from poor subtype selectivity, off-target toxicity, and drug resistance, severely restricting their clinical application. In contrast, allosteric sites feature low conservation, high hydrophobicity, weak polarity, confined spatial geometry, and dynamic cryptic properties. These characteristics endow allosteric modulators with distinct advantages including high selectivity, functional tunability, and improved safety, making allosteric therapy a key direction in modern drug discovery. MCE has curated nearly 1,000 structurally disclosed clinical-stage allosteric modulators. By analyzing allosteric protein–ligand complex structures from the PDB database, we extracted core pharmacophores and privileged scaffolds. Adopting a rational design strategy of “scaffold derivation + allosteric physicochemical filtering”, we performed secondary screening on the derived compounds strictly following the optimal physicochemical principles for allosteric binding based on universal allosteric pocket properties: molecular weight 300–500 Da, HBD ≤ 3, HBA = 3–8, PSA = 70–120 Å², rotatable bonds ≤ 6, highly rigid scaffolds, cLogP = 1.0–3.8, and no strongly ionizable groups. The selected compounds exhibit high rigidity and shape complementarity, making them well-suited for targeting shallow, dynamic, and hydrophobic-dominated allosteric pockets. This allosteric modulator library contains 4,315 structurally diverse, lead-like compounds dedicated to allosteric drug development, allosteric site targeting, and allosteric modulator screening. It is suitable for kinases, GPCRs, and other important drug targets. All compounds are analogs of clinical-stage allosteric modulators with a similarity score > 0.6, combining excellent druggability and allosteric binding potential. It provides a highly efficient tool for early-stage allosteric drug discovery.

Allosteric Modulator Lead‑like Compound Library

4315 compounds

Owing to the high conservation of orthosteric sites, conventional orthosteric drugs frequently suffer from poor subtype selectivity, off-target toxicity, and drug resistance, severely restricting their clinical application. In contrast, allosteric sites feature low conservation, high hydrophobicity, weak polarity, confined spatial geometry, and dynamic cryptic properties. These characteristics endow allosteric modulators with distinct advantages including high selectivity, functional tunability, and improved safety, making allosteric therapy a key direction in modern drug discovery.

MCE has curated nearly 1,000 structurally disclosed clinical-stage allosteric modulators. By analyzing allosteric protein–ligand complex structures from the PDB database, we extracted core pharmacophores and privileged scaffolds. Adopting a rational design strategy of “scaffold derivation + allosteric physicochemical filtering”, we performed secondary screening on the derived compounds strictly following the optimal physicochemical principles for allosteric binding based on universal allosteric pocket properties: molecular weight 300–500 Da, HBD ≤ 3, HBA = 3–8, PSA = 70–120 Å², rotatable bonds ≤ 6, highly rigid scaffolds, cLogP = 1.0–3.8, and no strongly ionizable groups. The selected compounds exhibit high rigidity and shape complementarity, making them well-suited for targeting shallow, dynamic, and hydrophobic-dominated allosteric pockets.

This allosteric modulator library contains 4,315 structurally diverse, lead-like compounds dedicated to allosteric drug development, allosteric site targeting, and allosteric modulator screening. It is suitable for kinases, GPCRs, and other important drug targets. All compounds are analogs of clinical-stage allosteric modulators with a similarity score > 0.6, combining excellent druggability and allosteric binding potential. It provides a highly efficient tool for early-stage allosteric drug discovery.

製品番号	製品名	Category	Target	構造式

HY-113138

3-Methyluridine 1 Publications Verification N3-Methyluridine	天然物 Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
3-Methyluridine (m ³U; N3-Methyluridine) is a methylated nucleotide present in ribosomal RNA (rRNA), mainly targeting specific base sites of RNA molecules such as 23S rRNA. 3-Methyluridine can introduce a methyl group at the N3 position of uracil, affecting the secondary structure stability and base pairing ability of RNA, and regulating ribosome function. For example, it affects ribosomal subunit binding and tRNA interaction. 3-Methyluridine is often used as a key raw material for the synthesis of modified nucleotides, and is used to construct RNA oligonucleotides containing methylation modifications to study the effects of RNA methylation on gene expression and drug resistance .

HY-113138R

3-Methyluridine (Standard) N3-Methyluridine (Standard)	Structural Classification 天然物 Endogenous metabolite Source Classification	Endogenous Metabolite Reference Standards
3-Methyluridine (Standard) is the analytical standard of 3-Methyluridine. This product is intended for research and analytical applications. 3-Methyluridine (m3U; N3-Methyluridine) is a methylated nucleotide present in ribosomal RNA (rRNA), mainly targeting specific base sites of RNA molecules such as 23S rRNA. 3-Methyluridine can introduce a methyl group at the N3 position of uracil, affecting the secondary structure stability and base pairing ability of RNA, and regulating ribosome function. For example, it affects ribosomal subunit binding and tRNA interaction. 3-Methyluridine is often used as a key raw material for the synthesis of modified nucleotides, and is used to construct RNA oligonucleotides containing methylation modifications to study the effects of RNA methylation on gene expression and drug resistance .

製品番号	製品名		Classification

HY-136426

Trifludimoxazin		Alkynes
Trifludimoxazin is a click chemistry reagent, a protoporphyrinogen oxidase (PPO) inhibitor and herbicide. Trifludimoxazin inhibits PPO, accumulates reactive oxygen species, damages cell membranes, and thereby causes weed death. Trifludimoxazin exhibits high-efficiency activity in controlling broadleaf weeds and grassy weeds .

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