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asinex-covalent-inhibitors-library

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (1) Autophagy (1) Bacterial (1) Biochemical Assay Reagents (1) CRFR (2) Endogenous Metabolite (1) GHSR (1) Histone Methyltransferase (1) iGluR (1) Notch (2) Opioid Receptor (1) PCSK9 (1) PKA (1) Ras (2) SOS1 (2) Wnt (1)
By Research Areas:	Cancer (6) Cardiovascular Disease (3) Endocrinology (3) Infection (2) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (2)

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Screening Libraries

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Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P2265A

SAH-SOS1A TFA	SOS1 Ras	Cancer
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-P2261

STAD 2	PKA	Infection
STAD 2 is a potent and selective disruptor of PKA-RII, with a K_d of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .

HY-P4153

Enlicitide chloride MK-0616 chloride	PCSK9	Cardiovascular Disease
Enlicitide chloride is an orally active inhibitor for PCSK9 that blocks the interaction between LPL receptor and PSCK9, with an IC₅₀ of 2.5 nM. Enlicitide chloride can be used in the study of cardiovascular diseases such as atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome or related cardiovascular and cardiometabolic disorders .

HY-P2203

SAHM1 1 Publications Verification	Notch	Inflammation/Immunology
SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice .

HY-P10488

cycFWRPW	Wnt Others	Cancer
cycFWRPW is a peptide inhibitor of TLE1. TLE1 is an oncogenic transcriptional co‐repressor that exerts its repressive effects through binding of transcription factors, and inhibits Wnt signaling .

HY-P2203A

SAHM1 TFA	Notch	Cancer
SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.

HY-P10212

AVLX-125 UCCB01-125	iGluR	Neurological Disease
AVLX-125 (UCCB01-125) is a PSD-95 and PDZ domain inhibitor with K_d value of 10 nM. AVLX-125 can be used in the study of inflammatory pain .

HY-P2265

SAH-SOS1A	SOS1 Ras	Cancer
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-125040

Isariin C	Endogenous Metabolite	Inflammation/Immunology
Isariin C is a flavonoid glycoside with antioxidant activity. Isariin C activates angiogenesis. Isariin C exhibits insecticidal activity in certain insects .

HY-P3223

Biphalin TFA	Opioid Receptor	Neurological Disease
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .

HY-P1368A

Stressin I TFA Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41) TFA	CRFR	Endocrinology
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, K_i is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats .

HY-P1368

Stressin I Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)	CRFR	Endocrinology
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a K_i of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats .

HY-B0671

Vancomycin Maximum Cited Publications 82 Publications Verification	Bacterial Autophagy Antibiotic	Infection Cancer
Vancomycin is an antibiotic for the treatment of bacterial infections.

HY-P2266

SAH-EZH2	Histone Methyltransferase	Cancer
SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .

HY-P1712A

Arthrofactin TFA	Biochemical Assay Reagents	Metabolic Disease
Arthrofactin (TFA) is an effective lipopeptide biosurfactant in Pseudomonas sp. MIS38. Arthrofactin (TFA) production is associated with multiple ATP dependent active transporter systems .

HY-P10964

Tezusomant	GHSR	Endocrinology
Tezusomant is a growth hormone receptor antagonist. Tezusomant is promising for research of diseases such as acromegaly caused by excessive growth hormone secretion .

Cat. No.	Product Name

HY-L0118V

*Asinex Covalent Inhibitors Library*	942 compounds
A unique set of molecules containing mild electrophilic moieties that covalently interact with amino acid residues in the target protein. The diversity of our compounds for covalent drug discovery ranges from natural product-like scaffolds to macrocycles, creating multiple opportunities in hit generation for a selected target.

Cat. No.	Product Name	Target	Research Area

HY-P2265A

SAH-SOS1A TFA	SOS1 Ras	Cancer
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-P2261

STAD 2	PKA	Infection
STAD 2 is a potent and selective disruptor of PKA-RII, with a K_d of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .

HY-N9526

Lyciumin B	Peptides	Cardiovascular Disease
Lyciumin B is a cyclic peptide isolated from Lysium chinense .

HY-P10488

cycFWRPW	Wnt Peptides	Cancer
cycFWRPW is a peptide inhibitor of TLE1. TLE1 is an oncogenic transcriptional co‐repressor that exerts its repressive effects through binding of transcription factors, and inhibits Wnt signaling .

HY-P2203A

SAHM1 TFA	Notch	Cancer
SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.

HY-P10212

AVLX-125 UCCB01-125	iGluR	Neurological Disease
AVLX-125 (UCCB01-125) is a PSD-95 and PDZ domain inhibitor with K_d value of 10 nM. AVLX-125 can be used in the study of inflammatory pain .

HY-P2265

SAH-SOS1A	SOS1 Ras	Cancer
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .

HY-P2192

JMV-320	Peptides	Others
JMV-320 is an active compound.

HY-125040

Isariin C	Endogenous Metabolite	Inflammation/Immunology
Isariin C is a flavonoid glycoside with antioxidant activity. Isariin C activates angiogenesis. Isariin C exhibits insecticidal activity in certain insects .

HY-P3223

Biphalin TFA	Opioid Receptor	Neurological Disease
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .

HY-P4153

Enlicitide chloride MK-0616 chloride	PCSK9	Cardiovascular Disease
Enlicitide chloride is an orally active inhibitor for PCSK9 that blocks the interaction between LPL receptor and PSCK9, with an IC₅₀ of 2.5 nM. Enlicitide chloride can be used in the study of cardiovascular diseases such as atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome or related cardiovascular and cardiometabolic disorders .

HY-P2203

SAHM1 1 Publications Verification	Notch	Inflammation/Immunology
SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice .

HY-P1368A

Stressin I TFA Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41) TFA	CRFR	Endocrinology
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, K_i is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats .

HY-P1368

Stressin I Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)	CRFR	Endocrinology
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a K_i of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats .

HY-B0671

Vancomycin Maximum Cited Publications 82 Publications Verification	Bacterial Autophagy Antibiotic	Infection Cancer
Vancomycin is an antibiotic for the treatment of bacterial infections.

HY-P2266

SAH-EZH2	Histone Methyltransferase	Cancer
SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .

HY-P1712A

Arthrofactin TFA	Biochemical Assay Reagents	Metabolic Disease
Arthrofactin (TFA) is an effective lipopeptide biosurfactant in Pseudomonas sp. MIS38. Arthrofactin (TFA) production is associated with multiple ATP dependent active transporter systems .

HY-P10014

Bibapcitide	Peptides	Cardiovascular Disease
Bibapcitide, a 26 amino acid, inhibits thrombosis .

HY-P10964

Tezusomant	GHSR	Endocrinology
Tezusomant is a growth hormone receptor antagonist. Tezusomant is promising for research of diseases such as acromegaly caused by excessive growth hormone secretion .

Lyciumin B	Cardiovascular Disease Alkaloids Classification of Application Fields Source classification Eupatorium triplinerve Vahl. Plants Solanaceae Lycium chinense Miller Disease Research Fields	Others
Lyciumin B is a cyclic peptide isolated from Lysium chinense .

Vancomycin 80+ Cited Publications	Infection Human Gut Microbiota Metabolites Plant Cell Culture Microorganisms Antibiotics Source classification Antibacterial Disease Research Endogenous metabolite Disease Research Fields Other Antibiotics Cancer	Bacterial Autophagy Antibiotic
Vancomycin is an antibiotic for the treatment of bacterial infections.

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asinex-covalent-inhibitors-library

Inhibitors & Agonists

Screening Libraries

Peptides

NaturalProducts

Natural
Products