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Results for "

selective chemical probe

" in MedChemExpress (MCE) Product Catalog:

By Targets:	17β-HSD (1) AAK1 (1) ADAMTS (1) Adrenergic Receptor (1) Akt (2) AMPK (1) Anaplastic lymphoma kinase (ALK) (2) Apoptosis (12) Arp2/3 Complex (2) Autophagy (7) Bcl-2 Family (1) Biochemical Assay Reagents (1) Calmodulin (1) Casein Kinase (1) Cathepsin (1) CCR (1) CDK (4) Cyclin G-associated Kinase (GAK) (1) Cytochrome P450 (1) DAPK (2) Deubiquitinase (2) Discoidin Domain Receptor (3) Disulfidptosis (2) DNA/RNA Synthesis (3) Dopamine Receptor (1) Drug Intermediate (1) DYRK (1) EBI2/GPR183 (1) Elastase (3) Endogenous Metabolite (1) Endonuclease (1) Endothelin Receptor (2) Epigenetic Reader Domain (32) ERK (3) FAAH (1) Farnesyl Transferase (1) Fatty Acid Synthase (FASN) (1) FKBP (2) Flavivirus (1) Fluorescent Dye (2) Glucocorticoid Receptor (1) GLUT (2) GnRH Receptor (1) GPR52 (2) GPR68 (1) GPR84 (1) GSK-3 (1) Haspin Kinase (1) HCV Protease (2) HDAC (1) Hippo (MST) (1) Histamine Receptor (2) Histone Acetyltransferase (5) Histone Methyltransferase (26) iGluR (1) IKK (1) Influenza Virus (1) IRAK (1) Isocitrate Dehydrogenase (IDH) (1) JAK (1) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (1) LIM Kinase (LIMK) (4) LRRK2 (2) MAGL (1) Mitochondrial Metabolism (1) MMP (4) Monocarboxylate Transporter (1) mTOR (1) Na+/H+ Exchanger (NHE) (1) Neuropeptide Y Receptor (2) P2X Receptor (1) P2Y Receptor (1) p38 MAPK (3) PAK (2) Phosphodiesterase (PDE) (1) PI5P4K (2) Prostaglandin Receptor (2) PROTACs (3) Reference Standards (20) RIP kinase (1) SRPK (1) TGF-beta/Smad (1) TGF-β Receptor (1) Tie (1) TNF Receptor (1) TRP Channel (2) Virus Protease (1) VSV (1) WDR5 (2) Wnt (2) γ-secretase (1)
By Research Areas:	Cancer (107) Cardiovascular Disease (6) Endocrinology (6) Infection (7) Inflammation/Immunology (28) Metabolic Disease (7) Neurological Disease (19)
Click Chemistry:	Alkynes (1)

171

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107455

A-485 Maximum Cited Publications 99 Publications Verification	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
A-485, a chemical probe, is a potent and selective catalytic inhibitor of p300/CBP with IC₅₀s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively .

HY-100411

MLi-2 10+ Cited Publications	LRRK2	Neurological Disease
MLi-2, a chemical probe, is an orally active and highly selective LRRK2 inhibitor with an IC₅₀ of 0.76 nM. MLi-2 has the potential for Parkinson’s disease .

HY-102080

SAFit2 5+ Cited Publications	FKBP	Cancer
SAFit2, a chemical probe, is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a K_i of 6 nM and also enhances AKT2-AS160 binding .

HY-13500

GSK343 30+ Cited Publications	Histone Methyltransferase Autophagy	Cancer
GSK343, a chemical probe, is a highly potent and selective EZH2 inhibitor with an IC₅₀ of 4 nM.

HY-18966

PF-04418948 10+ Cited Publications	Prostaglandin Receptor	Endocrinology Cancer
PF-04418948, a chemical probe, is an orally active, potent and selective prostaglandin EP₂ receptor antagonist with an IC₅₀ of 16 nM .

HY-119254

BAY-850 5 Publications Verification	Epigenetic Reader Domain	Metabolic Disease
BAY-850, a chemical probe, is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC₅₀ of 166 nM .

HY-101787

TP-024 2 Publications Verification FTBMT	GPR52	Neurological Disease
TP-024 (FTBMT), a chemical probe, is a selective GPR52 agonist with an EC₅₀ of 75 nM . TP-024 has antipsychotic and procognitive properties .

HY-19615

MS023 20+ Cited Publications	Histone Methyltransferase	Cancer
MS023, a chemical probe, is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC₅₀s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively .

HY-15646

UNC1999 10+ Cited Publications	Histone Methyltransferase Autophagy	Cancer
UNC1999, a chemical probe, is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC₅₀s of <10 nM and 45 nM, repectively.

HY-19715

SGC707 10+ Cited Publications	Histone Methyltransferase	Metabolic Disease
SGC707, a chemical probe, is a potent, selective, and non-competitive PRMT3 (protein arginine methyltransferase 3) inhibitor (IC₅₀=31 nM, K_d=53 nM).

HY-100235

GSK591 10+ Cited Publications EPZ015866; GSK3203591	Histone Methyltransferase	Cancer
GSK591 (EPZ015866), a chemical probe, is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC₅₀ of 4 nM .

HY-112445

SGC3027 5+ Cited Publications	Histone Methyltransferase	Cancer
SGC3027 is a histone methyltransferase inhibitor . SGC3027 is the first potent, selective and cell active chemical probe for PRMT7 .

HY-100018

BAY1125976 3 Publications Verification	Akt	Cancer
BAY1125976, a chemical probe, is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC₅₀ values of 5.2 nM and 18 nM at 10 μM ATP, respectively.

HY-19725

A-1155463 20+ Cited Publications	Bcl-2 Family	Cancer
A-1155463, a chemical probe, is a highly potent and selective BCL-XL inhibitor with an EC₅₀ of 70 nM in Molt-4 cell. A-1155463 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-100519

NVS-PAK1-1 5 Publications Verification	PAK	Cancer
NVS-PAK1-1, a chemical probe, is a potent and selective allosteric PAK1 inhibitor with an IC₅₀ of 5 nM .

HY-13980

UNC0642 20+ Cited Publications	Histone Methyltransferase	Cancer
UNC0642, a chemical probe, is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC₅₀ of <2.5 nM for G9a.

HY-102058

WM-1119 10+ Cited Publications	Histone Acetyltransferase	Cancer
WM-1119, a chemical probe, is a highly potent and selective KAT6A inhibitor, with an IC₅₀ of 0.25 μM for KAT6A in lymphoma cells, the binding K_D values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively .

HY-12409

PFI-3 5 Publications Verification	Epigenetic Reader Domain	Cancer
PFI-3, a chemical probe, is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a K_d of 89 nM.

HY-122186

SGC-GAK-1 2 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-107777

LLY-283 5+ Cited Publications	Histone Methyltransferase	Cancer
LLY-283, a chemical probe, is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC₅₀ of 22 nM and a K_d of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity .

HY-107725

BIBO3304 4 Publications Verification	Neuropeptide Y Receptor	Metabolic Disease
BIBO3304, a chemical probe, is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC₅₀=0.38 and 0.72 nM, respectively) .

HY-15300

Skepinone-L 2 Publications Verification CBS3830	p38 MAPK Autophagy	Inflammation/Immunology
Skepinone-L (CBS3830), a chemical probe, is a selective p38 mitogen-activated protein kinase inhibitor.

HY-19546

BAY-598 5+ Cited Publications	Histone Methyltransferase	Cancer
BAY-598, a chemical probe, is selective small molecule inhibitor of SMYD2 with an IC₅₀ of 27 nM .

HY-153045

BAY-805 3 Publications Verification	Deubiquitinase	Cancer
BAY-805, a chemical probe, is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes .

HY-14376

Redafamdastat 5+ Cited Publications PF-04457845	FAAH Autophagy	Neurological Disease
Redafamdastat (PF-04457845), a chemical probe, is a highly efficacious and selective FAAH inhibitor with IC₅₀ values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively.

HY-12681

CCT251545 3 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-15658

GSK2801 3 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
GSK2801, a chemical probe, is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with K_d values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4 .

HY-133117

BAY-985 4 Publications Verification	IKK	Cancer
BAY-985, a chemical probe, is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC₅₀s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy .

HY-130248

BAY-899 1 Publications Verification	GnRH Receptor	Endocrinology
BAY-899, a chemical probe, is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC₅₀s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels .

HY-19313

LLY-507 10+ Cited Publications	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-148814

BI-3231 2 Publications Verification	17β-HSD	Metabolic Disease
BI 3231, a chemical probe, is a potent and selective hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) inhibitor, with IC₅₀s of 1 and 13 nM for hHSD17B13 and mHSD17B13, respectively. BI 3231 has the potential for the research of nonalcoholic steatohepatitis (NASH) and other liver diseases .

HY-108886

JWG-071 5 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-100756

BAY-826 1 Publications Verification	Discoidin Domain Receptor Tie	Cancer
BAY-826, a chemical probe, is a selective and potent TIE-2 inhibitor with a K_d of 1.6 nM, respectively.

HY-16586

PFI-1 3 Publications Verification	Epigenetic Reader Domain Autophagy Apoptosis	Cancer
PFI-1, a chemical probe, is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC₅₀ of 0.22 μM in a cell-free assay.

HY-115506

PF-05105679	TRP Channel	Neurological Disease
PF-05105679, a chemical probe, is an orally active and selective TRPM8 antagonist with an IC₅₀ of 103 nM. PF-05105679 has the potential for cold-related pain .

HY-100220

GSK6853 2 Publications Verification	Epigenetic Reader Domain	Cancer
GSK6853, a chemical probe, is a potent and selective inhibitor of the BRPF1 bromodomain. GSK6853 shows excellent BRPF1 potency (pK_d = 9.5) and greater than 1600-fold selectivity over all other bromodomains .

HY-15649

UNC1215 4 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
UNC1215, a chemical probe, is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a K_d value of 120 nM and an IC₅₀ of 40 nM. UNC1215 has the potential to treat malignant brain tumor.

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-100518

T-26c 3 Publications Verification	MMP	Inflammation/Immunology
T-26c, a chemical probe, is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC₅₀ of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes .

HY-101125

L-Moses 2 Publications Verification L-45	Epigenetic Reader Domain	Cancer
L-Moses (L-45), a chemical probe, is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a K_d of 126 nM .

HY-124029

BI-4394 MMP13-IN-3	MMP	Inflammation/Immunology
BI-4394 (MMP13-IN-3), a chemical probe, is a potent, selective, and orally active MMP-13 inhibitor (IC₅₀=1 nM ) for the potential treatment of osteoarthritis . BI-4394 is >1000 selective over other MMPs .

HY-111457A

BAY-678 1 Publications Verification	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-137892

GSK620	Epigenetic Reader Domain	Inflammation/Immunology
GSK620, a chemical probe, is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .

HY-100352

BI-9564 2 Publications Verification	Epigenetic Reader Domain	Cancer
BI-9564, a chemical probe, is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC₅₀s of 75 nM and 3.4 μM and K_ds of 14 nM and 239 nM, respectively. BI-9564 has an IC₅₀ of > 100 μM for BET family .

HY-16100

BI 99179 3 Publications Verification	Fatty Acid Synthase (FASN)	Metabolic Disease Cancer
BI 99179, a chemical probe, is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC₅₀ of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats .

HY-139868

BAY-091	PI5P4K	Cancer
BAY-091, a chemical probe, is a potent and highly selective inhibitor of the kinase PIP4K2A.

HY-112082

BAY885 1 Publications Verification	ERK	Cancer
BAY885, a chemical probe, is a highly potent and selective ERK5 inhibitor with an IC₅₀ of 35 nM. BAY885 shows weak inhibition on others kinases .

HY-112080

BAY-6035	Histone Methyltransferase	Cancer
BAY-6035, a chemical probe, is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC₅₀ of 88 nM .

HY-145707

BAY-179	Mitochondrial Metabolism	Cancer
BAY-179, a chemical probe, is a potent, selective, and species cross-reactive complex I inhibitor. BAY-179 shows IC₅₀ values of 79 nM, 38 nM, 27 nM, and 47 nM for human, mouse, rat, and dog complex I, respectively .

Cat. No.	Product Name

HY-L063

Chemical Probe Library

281 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 281 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

5,994 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 5,994 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

1,546 compounds

MCE covalent inhibitor library contains 1,546 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

1,248 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

Non-natural Amino Acid Compound Library

134 compounds

Unlike the 20 natural amino acids commonly found within living organisms, non-natural 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, uon-natural 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.

HY-L945

Sulfonyl Fluoride Fragment Library

1162 compounds

Sulfonyl fluoride (-SO₂F) overcomes the bottleneck of target selectivity in traditional covalent warheads through its unique chemical and biological properties, which rely heavily on cysteine (Cys) residues. Featuring high stability and tunable electrophilicity under physiological conditions, it can target a wide range of nucleophilic residues including lysine (Lys), tyrosine (Tyr), serine (Ser), and histidine (His). It offers the advantages of a broader druggable space, lower off-target risks, and long-lasting efficacy, with numerous reported cases in the research of covalent inhibitors, Molecular glue, PROTACs, and chemical biology probe development.

MCE constructs a highly diverse sulfonyl fluoride fragment library based on the reactivity, stability and physiological compatibility of sulfonyl fluoride. The library contains 1000 efficiently synthesized and stable sulfonyl fluoride fragments, which ensure precise reactivity of the warhead and retain sufficient derivatization space for subsequent optimization. Combined with the modular strategy of SuFEx click chemistry, it enables versatile modification of compounds and functionalization of complex molecules, improves the efficiency of structural optimization and rapidly expands druggability, making it suitable for high-throughput probe and custom covalent library construction. It provides an efficient research tool for the development of broad-spectrum covalent inhibitors targeting Lys/Tyr/Ser/His, covalent PROTACs for E3 ligases and chemical biology probe development, meeting the requirements of modern drug research for high throughput, high success rate and high derivatization potential.

This library contains 1,162 sulfonyl fluoride fragments with high structural diversity, favorable drug-like properties and tunable electrophilicity. It is well suited for precise targeting of non-Cys residues and meets the criteria of simple structure and high derivatization potential. It effectively improves

Cat. No.	Product Name		Classification

HY-179099

WDR5 probe 1		Alkynes
Multi-target kinase-IN-8 (compound 16) is an efficient and highly selective WDR5 chemical probe. Multi-target kinase-IN-8 is a pharmaceutical intermediate. Multi-target kinase-IN-8 can be used for cancer research .

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