Search Result

Results for "

Reversible-covalent

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (1) Autophagy (1) Bacterial (1) Bcl-2 Family (1) Biochemical Assay Reagents (2) Btk (2) Cathepsin (1) CRFR (2) Dengue Virus (1) Dipeptidyl Peptidase (1) Drug Intermediate (1) Endogenous Metabolite (1) Enteropeptidase (1) Epigenetic Reader Domain (1) ERK (3) Flavivirus (1) GHSR (1) Histone Methyltransferase (2) IFNAR (1) iGluR (1) IKK (1) Interleukin Related (1) MAPKAPK2 (MK2) (1) Molecular Glues (2) NF-κB (1) Notch (2) Opioid Receptor (2) Parasite (1) PCSK9 (2) PERK (1) Phosphodiesterase (PDE) (1) PKA (1) PROTACs (1) Proteasome (1) Ras (2) Reference Standards (1) Renin (1) Ribosomal S6 Kinase (RSK) (2) SARS-CoV (7) SOS1 (2) STING (1) SULT (1) Toll-like Receptor (TLR) (1) Virus Protease (4) Wnt (1)
By Research Areas:	Cancer (20) Cardiovascular Disease (5) Endocrinology (3) Infection (11) Inflammation/Immunology (6) Metabolic Disease (4) Neurological Disease (6)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0671

Vancomycin Maximum Cited Publications 94 Publications Verification	Bacterial Autophagy Antibiotic	Infection Cancer
Vancomycin is an antibiotic for the treatment of bacterial infections.

HY-15816

Ulixertinib 45+ Cited Publications 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-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-112166

Rilzabrutinib 1 Publications Verification 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-15816A

Ulixertinib hydrochloride 45+ Cited Publications 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-172437

Secutrelvir S-892216	Virus Protease SARS-CoV	Infection
Secutrelvir is an oral SARS-CoV-2 3C-like protease (3CLpro) inhibitor and antiviral agent, with IC₅₀ values of 0.655 nM and 0.697 nM against SARS-CoV-2 3CLpro, respectively. Secutrelvir forms a reversible covalent bond with the catalytic cysteine C145 of SARS-CoV-2 3CLpro, thereby inhibiting viral replication. Secutrelvir exhibits activity against multiple SARS-CoV-2 variants and can be used in research related to coronavirus disease 2019 (COVID-19) .

HY-124704

Chst15-IN-1 1 Publications Verification	SULT	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-172615

AMPTX-1	Molecular Glues Epigenetic Reader Domain	Cancer
AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC₅₀ of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies .

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-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-W005118

2-Amino-4-fluoropyridine 4-Fluoropyridin-2-amine	Drug Intermediate	Cancer
2-Amino-4-fluoropyridine (4-Fluoropyridin-2-amine) is a drug intermediate that can be used for the synthesis reversible-covalent FGFR4 inhibitors .

HY-15816R

Ulixertinib (Standard) BVD-523 (Standard); VRT752271 (Standard)	ERK Reference Standards	Cancer
Ulixertinib (Standard) is the analytical standard of Ulixertinib. This product is intended for research and analytical applications. 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-P1368

Stressin I 1 Publications Verification 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-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-P1368A

Stressin I TFA 1 Publications Verification 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-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 .

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-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-P2261

STAD 2 1 Publications Verification	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-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 on diseases caused by excessive growth hormone secretion, such as acromegaly .

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-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-150717

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

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-178321

UNC10088	Molecular Glues Histone Methyltransferase	Cancer
UNC10088 is a molecular glue targeting NSD2. UNC10088 mediates the formation of a stable ternary complex between SCFFBXO22 and the NSD2 PWWP1 domain. UNC10088 promotes ubiquitination of the SCFFBXO22-dependent NSD2 PWWP1 domain through reversible covalent bonding with the C326 region of FBXO22. UNC10088 could be used in cancer research .

HY-P3223A

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

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-116533

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

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-120631A

BMS-538305 hydrochloride	Dipeptidyl Peptidase	Others
BMS-538305 hydrochloride is a potent and selective inhibitor of dipeptidyl peptidase IV (DPP-IV), exhibiting strong biological activity by forming a reversible covalent complex with the enzyme. BMS-538305 hydrochloride demonstrates its mechanism of action through the covalent attachment between the nitrile carbon of the inhibitor and the enzyme residue S630, as unveiled by the X-ray crystal structure analysis.

HY-123564

Mcl1-IN-7	Bcl-2 Family	Others
Mcl1-IN-7 (compound 11) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. By covalently targeting the non-catalytic lysine side chain of Mcl-1, it has higher potency than non-covalent counterparts and can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.

HY-116220

Mcl1-IN-14	Others	Others
Mcl1-IN-14 (compound 5) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. Mcl1-IN-14 covalently targets the non-catalytic lysine side chain of Mcl-1 and has higher potency than non-covalent counterparts, which can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.

HY-175712

SARS-CoV-2 Mpro-IN-47	SARS-CoV Virus Protease	Infection
SARS-CoV-2 Mpro-IN-47 is an orally active SARS-CoV-2 Mpro reversible covalent Inhibitor. SARS-CoV-2 Mpro-IN-47 shows potent antiviral activity against several clinical variants of SARS-CoV-2. SARS-CoV-2 Mpro-IN-47 can be used for the research of infection, such as SARS-CoV-2 .

HY-170649

RdRP-IN-9	SARS-CoV	Infection
RdRP-IN-9 (Compound 6b) is a reversible covalent allosteric inhibitor of RdRp. RdRP-IN-9 demonstrates high anti-coronavirus activity, with an EC₅₀ value of 0.68 μM against HCoV-OC43 RdRP-IN-9 exerts a more prolonged antiviral effect by reversibly acylating Cys12 in the NiRAN domain of non-structural protein 12 (nsp 12) and exhibits synergistic anti-coronavirus activity with Molnupiravir (HY-135853) .

HY-147927A

(S)-Human enteropeptidase-IN-1	Enteropeptidase	Metabolic Disease
(S)-Human enteropeptidase-IN-1 (Compound 6c) is an orally active enteropeptidase inhibitor with low systemic exposure (IC₅₀ (initial): 26 nM; IC₅₀ (app): 1.8 nM). (S)-Human enteropeptidase-IN-1 promotes increased fecal protein output and effectively reduces body weight in a diet-induced obese (DIO) rat model. (S)-Human enteropeptidase-IN-1 inhibits enteropeptidase via a reversible covalent mechanism and prolongs the enzyme inactivation time. (S)-Human enteropeptidase-IN-1 can be used in anti-obesity research .

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-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-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-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-179595

GSK4394835A	Phosphodiesterase (PDE)	Cardiovascular Disease
GSK4394835A is a reversible covalent inhibitor of PDE3B with a pIC₅₀ of 6.2. GSK4394835A can be used for cardiovascular disease research .

HY-183885

MPI3	SARS-CoV Virus Protease	Infection Inflammation/Immunology
MPI3 is a reversible covalent SARS-CoV-2 M_Pro inhibitor with an enzymatic IC₅₀ of 8.5 nM. MPI3 can be used for the research of covid-19 .

HY-180884

BTK-IN-46	Btk	Cancer
BTK-IN-46 (compound 24) is a reversible covalent BTK inhibitor. BTK-IN-46 covalently labels a lysine in the inositol phosphate (PIP3) binding site, thereby blocking Pleckstrin homology (PH) domain-mediated membrane recruitment and activation of BTK .

HY-180120

UM-203	STING IKK NF-κB IFNAR Interleukin Related	Inflammation/Immunology
UM-203 is a reversible covalent STING antagonist. UM-203 is effective against both mouse and human STING, and in particular, it inhibits the most common human STING R232 variant. UM-203 can inhibit STING oligomerization and reduce phosphorylation of downstream TBK1 and IRF3, thereby blocking the IRF3 and NF-κB-mediated signaling pathways and inhibiting IFNβ and IL-6 secretion. UM-203 can be used for the research of inflammation and immunology, such as systemic lupus erythematosus .

HY-180507

TLR2/9 antagonist 1	Toll-like Receptor (TLR)	Neurological Disease Inflammation/Immunology Cancer
TLR2/9 antagonist 1 (Compound 24) is a reversible covalent TLR2 (IC₅₀ = 0.5 μM (TLR2/TLR6); IC₅₀ = 0.6 μM (TLR2/TLR1)) and TLR9 (IC₅₀ = 0.32 μM) antagonist. TLR2/9 antagonist 1 has no significant effect on other TLR subtypes. TLR2/9 antagonist 1 can be used for studying central nervous system diseases and malignant tumors caused by inflammation .

HY-N17580

Lyciumin D	Renin	Cardiovascular Disease
Lyciumin D acts as an angiotensin-converting enzyme inhibitor and renin inhibitor. Lyciumin D can be used for the research of hypertension .

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-156052

CN-716 dihydrochloride	Flavivirus Dengue Virus Virus Protease	Infection
CN-716 dihydrochloride is a reversible covalent flavivirus NS2B·NS3 protease inhibitor with antiviral activity. CN-716 dihydrochloride effectively inhibits the replication of dengue virus (DENV2), West Nile virus (WNV) and Zika virus (ZIKV). The IC₅₀ values of CN-716 dihydrochloride against the proteases of the above three viruses are 0.066 μM, 0.11 μM and 0.25 μM, respectively, while the K_i values against the same proteases are 0.051 μM, 0.082 μM and 0.04 μM, respectively. CN-716 dihydrochloride can be used to study the infection mechanisms of dengue fever, West Nile fever and Zika virus infection .

HY-W1126955

Enlicitide (decanoate) MK-0616 (decanoate)	PCSK9	Metabolic Disease Inflammation/Immunology
Enlicitide (MK-0616) decanoate is an orally active macrocyclic peptide PCSK9 inhibitor. Enlicitide decanoate binds to PCSK9, blocks its interaction with low-density lipoprotein receptor (LDLR), and enhances hepatic clearance of LDL-C. Enlicitide decanoate reduces atherogenic lipoproteins, including non-HDL cholesterol, apolipoprotein B, and lipoprotein (a). Enlicitide decanoate is applicable to research related to hypercholesterolemia, heterozygous familial hypercholesterolemia, and atherosclerotic cardiovascular disease .

HY-P11837

NECT-224	Biochemical Assay Reagents	Cancer
NECT-224 is a bifunctional chelator and a nectin-4 targeting peptide conjugate. NECT-224 can be used as a PET imaging agent when labeled with ⁶⁴Cu or ⁶⁸Ga .

Cat. No.	Product Name

HY-L924

Boronic acid/boronic ester fragment library

1,488 compounds

Boronic acid and boronic ester represent a relatively novel and promising chemical structure in drug design. Boronic acid exists in an sp²-hybridized state, possessing an empty p-orbital that can act as a Lewis acid to accept lone pairs from heteroatoms (O, N, or S). This Lewis acidity enables it to form reversible covalent bonds with amino acid residues such as lysine, serine, threonine, and histidine. Currently, five FDA-approved drugs containing boronic acid or boronic ester predominantly involve such covalent binding mechanisms in their interactions with target proteins. Furthermore, boronic acid can serve as a bioisostere for carboxylic acids, phosphates, and phenolic groups, utilized to improve pharmacokinetic properties and enhance drug efficacy.

To date, five boron-containing drugs have been approved by the FDA. The unique properties of boronic acids and boronic esters confer significant potential in drug design, with applications spanning cancer therapy (e.g., multiple myeloma), anti-infectives (e.g., fungal infections, tuberculosis), anti-inflammatory treatments (e.g., atopic dermatitis), antibacterial agents (e.g., carbapenem-resistant bacterial infections), and Reactive Oxygen Species (ROS)-responsive prodrugs, among others. The MCE Boronic Acid/Boronic Ester Fragment Library, which contains 1,488 compounds, serves as a valuable tool for the development of boron-containing drugs.

Cat. No.	Product Name	Target	Research Area