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Reversible-covalent

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Btk (1) Cathepsin (1) CRFR (2) ERK (2) Histone Methyltransferase (1) iGluR (1) MAPKAPK2 (MK2) (1) Notch (2) Parasite (1) PERK (1) PKA (1) PROTACs (1) Proteasome (1) Ras (2) Ribosomal S6 Kinase (RSK) (2) SARS-CoV (3)
By Research Areas:	Cancer (10) Cardiovascular Disease (2) Endocrinology (3) Infection (5) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (3)

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112166

Rilzabrutinib PRN1008	Btk	Metabolic Disease Cancer
Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC₅₀ of 1.3 nM.

HY-144323

YF135	PROTACs PERK	Cancer
YF135 is an efficient and reversible-covalent KRAS ^G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS ^G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .

HY-116533

RMM-46

MAPKAPK2 (MK2) Cancer

RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases .
HY-157778

MK-7845

SARS-CoV Infection

MK-7845 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC₅₀ of 8.7 nM .
HY-146649

LmCPB-IN-1

Parasite Cathepsin Infection

LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pK_i of 9.7 .
HY-150717

RSK2-IN-3

Ribosomal S6 Kinase (RSK) Cancer

RSK2-IN-3 (Compound 26) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase .

RMM-46	MAPKAPK2 (MK2)	Cancer
RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases .

MK-7845	SARS-CoV	Infection
MK-7845 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC₅₀ of 8.7 nM .

LmCPB-IN-1	Parasite Cathepsin	Infection
LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pK_i of 9.7 .

RSK2-IN-3	Ribosomal S6 Kinase (RSK)	Cancer
RSK2-IN-3 (Compound 26) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase .

HY-148535

Calpain Inhibitor XI	Proteasome	Neurological Disease
Calpain Inhibitor XI is a reversible covalent inhibitor of calpain-1. Calpain Inhibitor XI can be used for the research of neurodegenerative disorders .

HY-152009

SARS-CoV-2 3CLpro-IN-7

SARS-CoV Infection

SARS-CoV-2 3CLpro-IN-7 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC₅₀ value of 1.4 µM .

SARS-CoV-2 3CLpro-IN-7	SARS-CoV	Infection
SARS-CoV-2 3CLpro-IN-7 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC₅₀ value of 1.4 µM .

HY-150643

RSK2-IN-2	Ribosomal S6 Kinase (RSK)	Cancer
RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase. RSK2-IN-2 is also described to inhibit MSK1, MSK2 and RSK3 .

HY-15816A

Ulixertinib hydrochloride Maximum Cited Publications 24 Publications Verification BVD-523 hydrochloride; VRT752271 hydrochloride	ERK	Cancer
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

HY-15816

Ulixertinib Maximum Cited Publications 24 Publications Verification BVD-523; VRT752271	ERK	Cancer
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

HY-124704

Chst15-IN-1	Others	Neurological Disease
Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair .

HY-152005

SARS-CoV-2 3CLpro-IN-6	SARS-CoV	Infection
SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro-IN-6 has potent inhibitory activity for SARS-CoV-2 3CL ^pro with an IC₅₀ value of 4.9 μM. SARS-CoV-2 3CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .

HY-P2203A

SAHM1 TFA	Notch
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-P2265

SAH-SOS1A	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-P2265A

SAH-SOS1A TFA	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-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-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-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-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-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-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 .

Cat. No.	Product Name	Target	Research Area

HY-P2265A

SAH-SOS1A TFA	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-P2203A

SAHM1 TFA	Notch
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-P2265

SAH-SOS1A	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-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-N9526

Lyciumin B

Peptides Cardiovascular Disease

Lyciumin B is a cyclic peptide isolated from Lysium chinense .

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

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-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-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-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-P10014

Bibapcitide

Peptides Cardiovascular Disease

Bibapcitide, a 26 amino acid, inhibits thrombosis .

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

HY-P10016

Pegmolesatide HS-20039; EPO-018B	Peptides	Endocrinology
Pegmolesatide(HS-20039; EPO-018B) a synthetic peptide-based erythropoiesis-stimulating agent, can be used for ??the study of anemia in chronic kidney disease .

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

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Reversible-covalent

Inhibitors & Agonists

Peptides

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Natural
Products