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Results for "

Irreversible covalent inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	17β-HSD (1) Apoptosis (8) Autophagy (1) Bacterial (1) Bcr-Abl (1) BMX Kinase (1) Btk (11) c-Kit (1) Calcium Channel (1) Cathepsin (2) CDK (4) Cholinesterase (ChE) (3) Deubiquitinase (1) DNA Methyltransferase (2) DNA/RNA Synthesis (1) E1/E2/E3 Enzyme (1) EGFR (11) Endogenous Metabolite (1) Epigenetic Reader Domain (1) FAAH (1) FAP (1) FGFR (4) Glutaminase (1) Glycosidase (1) GSK-3 (1) Histone Methyltransferase (3) HPV (1) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (3) Itk (1) JAK (1) MALT1 (1) MAPKAPK2 (MK2) (1) MEK (1) mTOR (1) NF-κB (1) Nucleoside Antimetabolite/Analog (2) Parasite (4) PDGFR (1) PDHK (1) PDI (1) Proteasome (2) Radionuclide-Drug Conjugates (RDCs) (1) Ras (7) Ribosomal S6 Kinase (RSK) (1) SARS-CoV (3) Src (1) SRPK (1) Virus Protease (3) YAP (1)
By Research Areas:	Cancer (63) Cardiovascular Disease (3) Endocrinology (1) Infection (8) Inflammation/Immunology (14) Neurological Disease (4)
Click Chemistry:	Azide (1) Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100944

Conduritol B epoxide 5+ Cited Publications	Glycosidase	Neurological Disease
Conduritol B epoxide is an irreversible covalently bound acid β-glucosidase (GCase) inhibitor.

HY-52101A

FMK 3 Publications Verification	Ribosomal S6 Kinase (RSK)	Cancer
FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.

HY-133740

MS117	Histone Methyltransferase	Cancer
MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC₅₀ of 18 nM .

HY-136605

DGY-06-116 2 Publications Verification	Src	Cancer
DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC₅₀ of 3nM. DGY-06-116 inhibits FGFR1 with an IC₅₀ of 8340 nM .

HY-102087

JPM-OEt 3 Publications Verification	Cathepsin	Cancer
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .

HY-163527

FGFR-IN-13	FGFR	Cancer
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC₅₀=0.20±0.02 nM) and FGFR4(IC₅₀=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .

HY-152232

BChE-IN-15	Cholinesterase (ChE)	Cancer
BChE-IN-15 (Compound 6) is a pseudo-irreversible and covalent BChE inhibitor with an IC₅₀ of 1.76 nM against hBChE .

HY-154975

SARS-CoV-2-IN-49	SARS-CoV	Others
SARS-CoV-2-IN-49 is an irreversible covalent inhibitor of SARS-CoV-2 main protease .

HY-161397

NA-1-157	Bacterial	Infection Inflammation/Immunology
NA-1-157 is a potent irreversible covalent inhibitor of the GES-5 carbapenemase, with a MIC of 0.5 μg/mL .

HY-18605

K-Ras G12C-IN-2	Ras	Cancer
K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.

HY-116856

SRPKIN-1 5 Publications Verification	SRPK	Cardiovascular Disease Cancer
SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC₅₀s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect .

HY-156105

8304-vs	Parasite Proteasome	Infection
8304-vs is a macrocyclic anti-Plasmodial agent that covalently and irreversibly targets the Plasmodium proteasome. 8304-vs effectively inhibits the growth of Plasmodium falciparum .

HY-43521

Ibrutinib-MPEA	Btk	Cancer
Ibrutinib-MPEA (Compound 20) is ibrutinib derivative. Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) that has been used to treat haematological malignancies .

HY-13943

CNX-774 1 Publications Verification	Btk	Cancer
CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC₅₀ of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification .

HY-19564

JX06 2 Publications Verification	PDHK Apoptosis	Cancer
JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC₅₀s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity .

HY-14645

(-)-DHMEQ 25+ Cited Publications Dehydroxymethylepoxyquinomicin	NF-κB	Inflammation/Immunology Cancer
(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity .

HY-114436

MRTX-1257 4 Publications Verification	Ras	Cancer
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

HY-101215

Evobrutinib 5+ Cited Publications M2951; MSC2364447C	Btk	Inflammation/Immunology Cancer
Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent BTK inhibitor, with an IC₅₀ of 8.9 nM. Evobrutinib (M2951) can be used for the research of autoimmune diseases .

HY-128867

bio-THZ1 1 Publications Verification	CDK	Cancer
bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC₅₀ of 3.2 nM .

HY-114304

COH000 1 Publications Verification	E1/E2/E3 Enzyme	Cancer
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC₅₀ of 0.2 μM for SUMOylation in vitro .

HY-153245

JNJ-64264681	Btk	Inflammation/Immunology Cancer
JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTK inhibitor. JNJ-64264681 exhibits good pharmacokinetic characteristics and can be used for cancer and autoimmune diseases research .

HY-18953

mTOR inhibitor-23	mTOR	Cancer
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .

HY-18930

NU6300	CDK	Cancer
NU6300 is a covalent, irreversible and ATP-competitive CDK2 inhibitor with an IC₅₀ value of 0.16 μM. NU6300 can be used for the research of eukaryotic cell cycle- and transcription-related .

HY-158378

Trivalent hydroxyarsinothricn R-AST-OH	Glutaminase	Cancer
Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy .

HY-W143698

PDGFRα kinase inhibitor 2	Bcr-Abl c-Kit PDGFR	Cancer
PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC₅₀s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1 wt, KIT wt, PDGFRR wt .

HY-151523

KRas G12R inhibitor 1	Ras	Cancer
KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research .

HY-133118

6RK73 2 Publications Verification	Deubiquitinase	Cancer
6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC₅₀ of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC₅₀=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer .

HY-P10828

MAPI	Virus Protease	Infection Inflammation/Immunology
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .

HY-141480

GSK-3β inhibitor 3	GSK-3 Apoptosis	Cancer
GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC₅₀ of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia .

HY-137028

2′-Thioadenosine PD157432	EGFR	Cancer
2'-Thioadenosine (PD157432) is a selective and irreversible inhibitor of ErbB-1 and ErbB-2, with an IC₅₀ of 45 µM for ErbB-2. 2'-Thioadenosine covalently inactivates ErbB-1 via modification of a cysteine residue at the active site .

HY-147250A

Lirafugratinib hydrochloride RLY-4008 hydrochloride	FGFR	Cancer
Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC₅₀ of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .

HY-147250

Lirafugratinib RLY-4008	FGFR	Cancer
Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC₅₀ of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .

HY-168050

nsP2 Protease-IN-1	Virus Protease	Infection
nsP2 Protease-IN-1 is a potent irreversible covalent inhibitor of Chikungunya (CHIKV) nsP2 cysteine protease with an IC₅₀ value of 60 nM. nsP2 Protease-IN-1 demonstrates potent antialphavirus activity, inhibiting CHIKV and VEEV replication with EC₅₀ = 0.01 and 0.3 µM, respectively .

HY-123891

NS-062	EGFR	Cancer
NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC₅₀ of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .

HY-145928

Divarasib 3 Publications Verification GDC-6036	Ras	Cancer
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC₅₀ of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

HY-125269

TED-347 5+ Cited Publications	YAP	Cancer
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC₅₀ of 5.9 μM for TEAD4?Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a K_i of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity .

HY-152108

SARS-CoV-2 Mpro-IN-6	SARS-CoV	Infection
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M ^pro inhibitor with an IC₅₀ of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .

HY-164002

PF-303	Btk	Others
PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC₅₀=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation .

HY-14380

PF-3845 1 Publications Verification	FAAH Autophagy	Inflammation/Immunology Cancer
PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a K_i of 0.23 μM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition .

HY-112161

Branebrutinib 2 Publications Verification BMS-986195	Btk	Cancer
Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC₅₀ of 0.1 nM . Branebrutinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-145928B

Divarasib adipate GDC-6036 adipate	Ras	Cancer
Divarasib (GDC-6036) adipate is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC₅₀ of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state .

HY-114436S

MRTX-1257-d6	Isotope-Labeled Compounds	Cancer
MRTX-1257-d₆ is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

HY-124069

M-525	Epigenetic Reader Domain	Cancer
M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC₅₀ of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity .

HY-15771

Tirabrutinib 5 Publications Verification ONO-4059; GS-4059	Btk Apoptosis	Inflammation/Immunology Cancer
Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC₅₀ of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies .

HY-15771A

Tirabrutinib hydrochloride 5 Publications Verification ONO-4059 hydrochloride; GS-4059 hydrochloride	Btk Apoptosis	Inflammation/Immunology Cancer
Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC₅₀ of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies .

HY-15772

Osimertinib Maximum Cited Publications 122 Publications Verification AZD-9291; Mereletinib	EGFR	Cancer
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-15772A

Osimertinib mesylate Maximum Cited Publications 122 Publications Verification AZD-9291 mesylate; Mereletinib mesylate	EGFR	Cancer
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-15772S1

Osimertinib-13C,d3 AZD-9291-¹³C,d₃; Mereletinib-¹³C,d₃	EGFR	Cancer
Osimertinib- ¹³C,d₃ is the deuterium and ¹³C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.

HY-116090

Conoidin A	Parasite	Infection Cardiovascular Disease Neurological Disease
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC₅₀ of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII) . Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease .

HY-164725

FAPI-mFS	Radionuclide-Drug Conjugates (RDCs) FAP	Cancer
FAPI-mFS is an irreversible fibroblast activation protein (FAP) inhibitor, that enhances the uptake and retention time in cancer cells through its covalent binding property for FAP. FAPI-mFS can be used for cancer imaging the therapy, when labeled with radioactive 68Ga or 177Lu . FAPI-mFS can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

Cat. No.	Product Name

HY-L036

Covalent Screening Library

1,450 compounds

Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.

MCE covalent inhibitor library contains 1,450 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

HY-L036P

Covalent Screening Library Plus

5,738 compounds

MCE covalent inhibitor library contains 5,738 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

HY-L908

Lead-like Covalent Screening Library

1,049 compounds

MCE Lead-like Covalent Screening Library offers a valuable resource of 1,049 lead-like compounds with commonly used covalent warheads. These warheads, such as acrylamide, activated terminal alkyne, acyloxymethyl ketone, and boronic acid, are capable of reacting with specific amino acid residues, including cysteine, lysine, serine, and histidine. The inclusion of these reactive warheads in the library allows researchers to explore the potential of covalent inhibition, a powerful approach in drug discovery.

Cat. No.	Product Name	Target	Research Area

HY-164725

FAPI-mFS	Radionuclide-Drug Conjugates (RDCs) FAP	Cancer
FAPI-mFS is an irreversible fibroblast activation protein (FAP) inhibitor, that enhances the uptake and retention time in cancer cells through its covalent binding property for FAP. FAPI-mFS can be used for cancer imaging the therapy, when labeled with radioactive 68Ga or 177Lu . FAPI-mFS can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

HY-P10828

MAPI	Virus Protease	Infection Inflammation/Immunology
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .

HY-P10428

E6AP-mimicking peptide	HPV	Infection
E6AP-mimicking peptide (compound 13) is a high-affinity, selective, irreversible and potent peptide-based covalent HPV16 E6 inhibitor targeting the 16E6 oncoprotein using a cysteine-reactive acrylamide warhead. E6AP-mimicking peptide has a K_i of 17 nM. E6AP-mimicking peptide targets all residues appearing in the binding pocket of E6 to disrupt the binding interface of 16E6 and E6AP. E6AP-mimicking peptide selectively binds and crosslinks to MBP-16E6 in PBS or a protein mixture .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13821

Epoxomicin 10+ Cited Publications BU-4061T	Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Inflammation/Immunology Disease Research Fields	Proteasome Apoptosis
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity .

HY-100196AR

Pyrroloquinoline quinone (disodium salt) (Standard)	Quinones Structural Classification Microorganisms Source classification Benzene Quinones Endogenous metabolite	Endogenous Metabolite
Triazophos (Standard) is the analytical standard of Triazophos. This product is intended for research and analytical applications. Triazophos, a non-systemic insecticide and acaricide that acts as an acetylcholinesterase (AChE) inhibitor, covalently and irreversibly binds to the acetylcholine binding site, thus blocking the hydrolysis of acetylcholine and leading to hyperexcitability; it is effective against a variety of soil insects and mites, including aphids, thrips, midges, beetles, Lepidoptera larvae, cutworms, and spider mites in crops such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee.

Cat. No.	Product Name	Chemical Structure

HY-15772S1

Osimertinib-13C,d3
Osimertinib- ¹³C,d₃ is the deuterium and ¹³C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.

HY-15772S

Osimertinib-d6
Osimertinib-d₆ is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

HY-114436S

MRTX-1257-d6
MRTX-1257-d₆ is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

HY-W757743

Acalabrutinib-d3
Acalabrutinib-d₃ (ACP-196-d₃) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).

HY-114277S

Sotorasib-d7

Sotorasib-d₇ (AMG-510-d₇) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .

Cat. No.	Product Name		Classification

HY-100433

PACMA 31		Alkynes
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC₅₀ of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues . PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-134318B

8-Azido-ADP disodium		Azide
8-Azido-ADP (disodium) is a covalent-binding inhibitor of mitochondrial adenine nucleotide translocation. 8-Azido-ADP (disodium) causes irreversible inhibition of adenine nucleotide exchange in a light-dependent reaction. 8-Azido-ADP (disodium) inhibits the normal state 4 → 3 transitions of mitochondrial respiration induced by ADP . 8-Azido-ADP (disodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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