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Results for "

selective chemical probe

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Biochemical Assay Reagents (1) Casein Kinase (1) CDK (2) Cyclin G-associated Kinase (GAK) (1) DNA/RNA Synthesis (1) DYRK (1) EBI2/GPR183 (1) Elastase (2) Endogenous Metabolite (1) Epigenetic Reader Domain (7) ERK (1) Eukaryotic Initiation Factor (eIF) (1) Fluorescent Dye (2) GPR84 (1) Histone Methyltransferase (4) LIM Kinase (LIMK) (2) PROTACs (1) Wnt (1)
By Research Areas:	Cancer (20) Inflammation/Immunology (6) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-108886

JWG-071 3 Publications Verification	ERK	Cancer
JWG-071 is the kinase-selective chemical probe for ERK5. JWG-071 inhibits ERK5 and LRRK2 with IC₅₀ values of 88nM and 109 nM, respectively .

HY-151813

NNMT-IN-4	Fluorescent Dye	Cancer
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC₅₀ values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .

HY-112445

SGC3027 3 Publications Verification	Histone Methyltransferase	Cancer
SGC3027 is a histone methyltransferase inhibitor . SGC3027 is the first potent, selective and cell active chemical probe for PRMT7 .

HY-122186

SGC-GAK-1 1 Publications Verification	Cyclin G-associated Kinase (GAK)	Cancer
SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a K_i of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK .

HY-12681

CCT251545 2 Publications Verification	Wnt	Cancer
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC₅₀ of 5 nM in 7dF3 cells . CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease .

HY-111457A

BAY-678	Elastase	Inflammation/Immunology
BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC₅₀ of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

HY-112803

GNE-371	DNA/RNA Synthesis	Cancer
GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC₅₀ of 10 nM for TAF1(2).

HY-149761

GSK023	Epigenetic Reader Domain	Others
GSK023 (compound 31) is a selective chemical probe targeting the BET BD1 domain .

HY-169295

RAP 1	Biochemical Assay Reagents	Others
RAP 1 is a reactive affinity probe (RAP) that selectively labels SLC6A8 in the presence of guanine alanine (GPA). RAP 1 can be used as a chemical probe for identifying and studying potential drug binding sites on SLC6A8 .

HY-126346

DL-175	GPR84	Inflammation/Immunology
DL-175 (compound 13) is a selective GPR84 agonist with biased agonistic activity. DL-175 can selectively activate functional responses in immune cells and induce enhanced chemotaxis and phagocytosis of human bone marrow cells. DL-175 is a potential chemical probe .

HY-134673A

UZH1a 2 Publications Verification	Apoptosis	Cancer
UZH1a is a potent and selective METTL3 inhibitor, with an IC₅₀ of 280 nM. UZH1a can be used for epitranscriptomic modulation of cellular processes. UZH1a has antitumor activity. UZH1a also can be used as a chemical probe for studying METTL3 .

HY-116814

ML401	EBI2/GPR183	Inflammation/Immunology
ML401, a potent chemical probe, selectively antagonizes EBI2 (also known as GPR183) with an IC₅₀ of 1.03 nM. ML401 displays activity in a chemotaxis assay (IC₅₀=6.24 nM). ML401 shows good stability and no toxicity .

HY-111515

BAY-678 racemate	Elastase	Inflammation/Immunology
BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC₅₀ of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

HY-124660A

A-395N	Endogenous Metabolite	Others
A-395N serves as a control probe for A-395, a highly potent and selective chemical probe targeting the polycomb protein EED, a key player in Polycomb repressive complex 2 (PRC2) responsible for transcriptional repression via histone H3K27 methylation. While A-395N bears structural similarities to A-395, it demonstrates no pharmacological activity in biochemical or cellular assays, making it an ideal control compound.

HY-116255

MS453	Histone Methyltransferase	Others
MS453 is a potent and highly selective SETD8 inhibitor with an IC50 value of 804 nM. MS453 specifically modifies a cysteine residue close to the inhibitor binding site. MS453 is selective for 28 other methyltransferases. The crystal structure of MS453 reveals its binding mode to SETD8, providing an atomic-level view for the development of high-quality chemical probes for SETD8 .

HY-137346

DD-03-156 (S,R,S)-AHPC-Me-PEG2-dabrafenib	PROTACs CDK LIM Kinase (LIMK)	Cancer
DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17 (Blue: VHL ligand (HY-112078), Black: linker HY-124380 (HY-124380)；Pink: BRAF inhibitor (HY-14660)) .

HY-111457

BAY-677	Others	Inflammation/Immunology
BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC₅₀ of 20 nM . BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC) .

HY-19313

LLY-507 Maximum Cited Publications 8 Publications Verification	Histone Methyltransferase	Cancer
LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC₅₀ <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes .

HY-132308

DYRK1-IN-1 2 Publications Verification	DYRK	Neurological Disease
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC₅₀ value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe .

HY-33838

eIF4A3-IN-8	Eukaryotic Initiation Factor (eIF)	Cancer
eIF4A3-IN-8 is a selective ATP-competitive eukaryotic initiation factor 4A3 (eIF4A3) inhibitor. eIF4A3-IN-8 can serve as a valuable chemical probe to elucidate the detailed function of eIF4A3 and EJC (exon junction complex) .

HY-19336

BAZ2-ICR 1 Publications Verification	Epigenetic Reader Domain	Cancer
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC₅₀s of 130 nM and 180 nM, and K_ds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe .

HY-114204

GSK8814	Epigenetic Reader Domain	Cancer
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pK_d=8.1 and a pK_i=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC₅₀s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1 .

HY-101121

NI-42	Epigenetic Reader Domain	Cancer
NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC₅₀s of BRPF1/2/3=7.9/48/260 nM; K_ds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins .

HY-18975

I-BRD9 5 Publications Verification	Epigenetic Reader Domain	Inflammation/Immunology Cancer
I-BRD9 is a selective cellular **chemical probe of bromodomain-containing protein 9 (BRD9) with pIC₅₀** value of 7.3 μM. I-BRD9 has high selectivity for bromodomain and extra terminal domain (BET) family and highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 can be used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways .

HY-100201

A-196 5 Publications Verification	Histone Methyltransferase	Cancer
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC₅₀ values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .

HY-112804

SGC-iMLLT 1 Publications Verification	Epigenetic Reader Domain	Cancer
SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC₅₀ of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with K_ds of 0.129 and 0.077 μM, respectively .

HY-134673

UZH1 3 Publications Verification	Apoptosis	Cancer
UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor, with an IC₅₀ of 280 nM. UZH1b (IC₅₀=28 µM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. UZH1 has antitumor activity. UZH1 also can be used as a chemical probe for studying METTL3 .

HY-139004

SGC-CK2-1 1 Publications Verification	Casein Kinase	Neurological Disease
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC₅₀s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases .

HY-122630

TH-257	LIM Kinase (LIMK)	Cancer
TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC₅₀ values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM .

HY-112626

CDK12-IN-2	CDK	Cancer
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC₅₀=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .

HY-135985

DCLK1-IN-1 1 Publications Verification	Fluorescent Dye	Cancer
DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC₅₀: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 ⁺ pancreatic ductal adenocarcinoma (PDAC) .

HY-149026

GNE-064	Epigenetic Reader Domain	Others
GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC₅₀ of 0.035 μM and inhibits SMARCA2 with an EC₅₀ of 0.10 μM. GNE-064 possess K_ds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis .

Cat. No.	Product Name

HY-L063

Chemical Probe Library	277 compounds
Chemical probes are simply reagents with high potency, selectivity and cell-permeability which play important roles in both fundamental and applied biological research. In their most common application, chemical probes can establish the tractability of a specific target. They are used to interrogate the relationship between a target and its phenotype (biological tractability) as well as an ability to modulate that phenotype using a small molecule. Otherwise, chemical probes also have had a major impact in enabling and accelerating discoveries along the path to pioneer medicines. They have helped to improve the understanding of targets and pathways and have created opportunities for proprietary drug discovery efforts to an extent that would not have been possible otherwise. MCE provides a unique collection of 277 chemical probes with high potency (at least 100 nM potency), selectivity (at least 10-fold selectivity against any other target) and cell-permeability (at least 10 μM potency). MCE Chemical probe library is a useful tool for target identification and mechanism research.

Chemical Probe Library

277 compounds

Chemical probes are simply reagents with high potency, selectivity and cell-permeability which play important roles in both fundamental and applied biological research. In their most common application, chemical probes can establish the tractability of a specific target. They are used to interrogate the relationship between a target and its phenotype (biological tractability) as well as an ability to modulate that phenotype using a small molecule. Otherwise, chemical probes also have had a major impact in enabling and accelerating discoveries along the path to pioneer medicines. They have helped to improve the understanding of targets and pathways and have created opportunities for proprietary drug discovery efforts to an extent that would not have been possible otherwise.

MCE provides a unique collection of 277 chemical probes with high potency (at least 100 nM potency), selectivity (at least 10-fold selectivity against any other target) and cell-permeability (at least 10 μM potency). MCE Chemical probe library is a useful tool for target identification and mechanism research.

HY-L036P

Covalent Screening Library Plus	5,763 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 5,763 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.

Covalent Screening Library Plus

5,763 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 5,763 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-L036

Covalent Screening Library	1,467 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 1,467 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.

Covalent Screening Library

1,467 compounds

MCE covalent inhibitor library contains 1,467 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-L908

Lead-like Covalent Screening Library	1,049 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 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.

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.

HY-L198

Unnatural Amino Acid Compound Library	129 compounds
Unlike the 20 natural amino acids commonly found within living organisms, unnatural amino acids are synthesized through chemical or biosynthetic methods, thereby being endowed with unique chemical properties or biological activities. In drug development, these amino acids can be utilized to design novel pharmaceutical molecules that may exhibit superior pharmacological characteristics, such as increased selectivity, improved pharmacokinetic profiles, or reduced toxicity. In biomedical research, unnatural amino acids can act as biological markers or probes for investigating biological processes like cell signaling, protein conformation, and protein-protein interactions. In addition, non-natural amino acids can also be used in the field of agriculture to develop new pesticides, plant growth regulators and so on. MCE included 129 unnatural amino acids and relative derivatives, serving as valuable tools for drug development and pesticide research.

Unnatural Amino Acid Compound Library

129 compounds

Unlike the 20 natural amino acids commonly found within living organisms, unnatural amino acids are synthesized through chemical or biosynthetic methods, thereby being endowed with unique chemical properties or biological activities. In drug development, these amino acids can be utilized to design novel pharmaceutical molecules that may exhibit superior pharmacological characteristics, such as increased selectivity, improved pharmacokinetic profiles, or reduced toxicity. In biomedical research, unnatural amino acids can act as biological markers or probes for investigating biological processes like cell signaling, protein conformation, and protein-protein interactions. In addition, non-natural amino acids can also be used in the field of agriculture to develop new pesticides, plant growth regulators and so on.

MCE included 129 unnatural amino acids and relative derivatives, serving as valuable tools for drug development and pesticide research.

Cat. No.	Product Name	Type

HY-112803

GNE-371	Fluorescent Dyes/Probes
GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC₅₀ of 10 nM for TAF1(2).

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