Search Result

Results for "

Aberrant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AAK1 (2) Aldose Reductase (1) Apoptosis (5) ATM/ATR (1) Aurora Kinase (1) Bcr-Abl (1) Btk (2) CaMK (1) CDK (4) Cyclin G-associated Kinase (GAK) (2) Epigenetic Reader Domain (1) Ferroptosis (2) Histone Demethylase (3) JAK (1) LIM Kinase (LIMK) (3) MALT1 (1) MAP4K (1) MAPKAPK2 (MK2) (1) Microtubule/Tubulin (2) Mucin (1) Phosphatase (1) PKC (1) PPAR (1) PROTACs (3) Proteasome (2) Pyruvate Kinase (1) ROCK (1) ROR (1) Salt-inducible Kinase (SIK) (3) SHP2 (1) TNF Receptor (1) ULK (2) Wee1 (2)
By Research Areas:	Cancer (16) Cardiovascular Disease (2) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (5)

By Targets:

AAK1 (2)

Aldose Reductase (1)

Apoptosis (5)

ATM/ATR (1)

Aurora Kinase (1)

Bcr-Abl (1)

Btk (2)

CaMK (1)

CDK (4)

Cyclin G-associated Kinase (GAK) (2)

Epigenetic Reader Domain (1)

Ferroptosis (2)

Histone Demethylase (3)

JAK (1)

LIM Kinase (LIMK) (3)

MALT1 (1)

MAP4K (1)

MAPKAPK2 (MK2) (1)

Microtubule/Tubulin (2)

Mucin (1)

Phosphatase (1)

PKC (1)

PPAR (1)

PROTACs (3)

Proteasome (2)

Pyruvate Kinase (1)

ROCK (1)

ROR (1)

Salt-inducible Kinase (SIK) (3)

SHP2 (1)

TNF Receptor (1)

ULK (2)

Wee1 (2)

By Research Areas:

Cancer (16)

Cardiovascular Disease (2)

Inflammation/Immunology (3)

Metabolic Disease (1)

Neurological Disease (5)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148324

PKM2 activator 5	Pyruvate Kinase	Cancer
PKM2 activator 5 (compound 8) is a PKM2 activator with an AC₅₀ value of 0.316 µM. PKM2 activator 5 has the potential to alter the aberrant metabolism of cancer cells .

HY-148062

RSS0680	PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1	Others
RSS0680 (Example 22) is a bifunctional compound targeted protein degradation of kinases. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used for research of disease or disorder mediated by aberrant kinase activity .

HY-148063

DB0614	PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) ULK Wee1 LIM Kinase (LIMK)	Others
DB0614 (Example 21) is a bifunctional compound targeted protein degradation of kinases. DB0614 degrades AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .

HY-148061

DB1113	PROTACs Bcr-Abl CDK Salt-inducible Kinase (SIK) Cyclin G-associated Kinase (GAK) MAP4K MAPKAPK2 (MK2) Ferroptosis ULK LIM Kinase (LIMK)	Others
DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity .

HY-157941

ART0380	ATM/ATR	Cancer
ART0380 is a potent and selective ATR kinase inhibitor. ART0380 has selective antitumor activity that can be used for the research of Ataxia-Telangiectasia Mutated (ATM) aberrant cancers .

HY-138830

TAK-418	Histone Demethylase	Neurological Disease
TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC₅₀ of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models .

HY-111425

SSE15206	Microtubule/Tubulin Apoptosis	Cancer
SSE15206 is a microtubule polymerization inhibitor (GI₅₀ = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells .

HY-P2508

MUC1, mucin core	Mucin	Cancer
MUC1, mucin core is the region of the MUC1 mucin core. MUC1 is a type I transmembrane glycoprotein, and is overexpressed and aberrantly glycosylated in carcinoma cells. MUC1, mucin core protein binds to domain 1 of ICAM-1 .

HY-13649

Indibulin ZIO 301; D 24851	Microtubule/Tubulin Apoptosis	Neurological Disease Cancer
Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .

HY-151192

LSD1/2-IN-3	Histone Demethylase	Cancer
LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a K_i value of 11 nM instead of 7 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation .

HY-15771A

Tirabrutinib hydrochloride 3 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-15771

Tirabrutinib 3 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-134471

TNF-α-IN-2 1 Publications Verification	TNF Receptor	Inflammation/Immunology
TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC₅₀ of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis .

HY-143432A

(S)-Cdc7-IN-18	CDK	Cancer
(S)-Cdc7-IN-18 is a potent inhibitor of CDC7. Overexpression of huCdc7 promotes overactivation of MCM2, an important marker of tumor cells, and thus promotes aberrant proliferation of tumor cells. (S)-Cdc7-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2020239107A1, compound 1-1) .

HY-123099

MS-1020	JAK	Cancer
MS-1020 is a potent and ATP-competitive JAK3 inhibitor. MS-1020 inhibits JAK3/STAT signaling and induces apoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylated STAT3 levels. MS-1020 has the potential for the research of cancers harboring aberrant JAK3 signaling .

HY-125639

(rac)-AR-13503 (rac)-AR-13324 M1 metabolite	PKC ROCK	Cardiovascular Disease
(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice .

HY-142648A

(R)-MLT-985	MALT1	Cancer
(R)-MLT-985 (compound 11) is a potent MALT1 protease inhibitor with an IC₅₀ of 3 nM. (R)-MLT-985 has an IC₅₀ of 20 nM for MALT1-dependent IL-2 production in Jurkat cells. (R)-MLT-985 suppresses growth and aberrant CARD11/BCL10/MALT1 complex signaling in ABC-DLBCL cells .

HY-106198

Lidorestat IDD-676	Aldose Reductase	Metabolic Disease
Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC₅₀ of 5 nM. Lidorestat can be used for chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation .

HY-143300

BRD4-BD1-IN-2	Epigenetic Reader Domain	Cardiovascular Disease Cancer
BRD4-BD1-IN-2 is a selective BRD4-BD1 inhibitor, with an IC₅₀ of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases .

HY-151190

cis-4-Br-2,5-F2-PCPA S1024	Histone Demethylase	Cancer
cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a K_i value of 94 nM instead of 8.4 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells .

HY-136173

Batoprotafib 2 Publications Verification TNO155	SHP2 Phosphatase	Cancer
Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC₅₀=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors .

HY-139534

ARI-1	ROR Apoptosis	Cancer
ARI-1 is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 effectively inhibits aberrant ROR1 expression, which is associated with the development of non-small cell lung cancer (NSCLC) and EGFR-TKI-induced drug resistance. ARI-1 binds to the extracellular Frizzled domain of ROR1 and regulates PI3K/AKT/mTOR signaling in a ROR1-dependent manner. ARI-1 potently inhibits NSCLC cell proliferation and migration and has antitumor activity in vivo ^{[1] ^.}

HY-109001

Alicapistat 1 Publications Verification ABT-957	Proteasome	Neurological Disease
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC₅₀ value of 395 nM .

HY-109001A

(1S,2R)-Alicapistat (1S,2R)-ABT-957	Proteasome	Neurological Disease
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC₅₀ value of 395 nM .

HY-145804

AZD-9574 1 Publications Verification	PPAR	Neurological Disease
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD ⁺ breast cancer and advanced solid malignancies research .

Cat. No.	Product Name

HY-L123

Human Metabolite Library	5970 compounds
Human metabolism is an integral part of cellular function that reflects individual differences in health, disease, diet, and lifestyle. Many health conditions such as obesity, diabetes, hypertension, heart disease, and cancer are associated with abnormal metabolic states. In the pathological state of the human body, metabolic pathways are significantly altered, resulting in aberrant levels of intermediates or end-products that can be viewed as potential diagnostic biomarkers or even therapeutic targets. Therefore, detection, identification and quantification of human metabolites are very important for drug metabolism research in drug development. MCE offers a unique collection of 5970 human metabolites, including endogenous metabolites and exogenous metabolites, covering multiple structure types, such as lipids, amino acids, nucleic acids, carbohydrates, organic acids, biogenic amines, vitamins,. MCE Human Metabolites Library is a helpful tool for studying the relationship between diseases and metabolism.

Human Metabolite Library

5970 compounds

Human metabolism is an integral part of cellular function that reflects individual differences in health, disease, diet, and lifestyle. Many health conditions such as obesity, diabetes, hypertension, heart disease, and cancer are associated with abnormal metabolic states. In the pathological state of the human body, metabolic pathways are significantly altered, resulting in aberrant levels of intermediates or end-products that can be viewed as potential diagnostic biomarkers or even therapeutic targets. Therefore, detection, identification and quantification of human metabolites are very important for drug metabolism research in drug development.

MCE offers a unique collection of 5970 human metabolites, including endogenous metabolites and exogenous metabolites, covering multiple structure types, such as lipids, amino acids, nucleic acids, carbohydrates, organic acids, biogenic amines, vitamins,. MCE Human Metabolites Library is a helpful tool for studying the relationship between diseases and metabolism.

HY-L020

Wnt/Hedgehog/Notch Compound Library	349 compounds
The developmental proteins Hedgehog, Notch and Wnt are key regulators of cell fate, proliferation, migration and differentiation in several tissues. Their related signaling pathways are frequently activated in tumors, and particularly in the rare subpopulation of cancer stem cells. The Wnt signaling pathway is a conserved pathway in animals. Deregulated Wnt signaling has catastrophic consequences for the developing embryo and it is now well appreciated that defective Wnt signaling is a causative factor for a number of pleiotropic human pathologies, including cancer. Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. The Notch signaling pathway is a highly conserved cell signaling system present in most animals. It plays an important role in cell-cell communication, and further regulates embryonic development. MCE designs a unique collection of 349 Wnt/Hedgehog/Notch signaling pathway-related small molecules. Wnt/Hedgehog/Notch Compound Library serves as a useful tool for stem cell research and anti-cancer drug screening.

Wnt/Hedgehog/Notch Compound Library

349 compounds

The developmental proteins Hedgehog, Notch and Wnt are key regulators of cell fate, proliferation, migration and differentiation in several tissues. Their related signaling pathways are frequently activated in tumors, and particularly in the rare subpopulation of cancer stem cells. The Wnt signaling pathway is a conserved pathway in animals. Deregulated Wnt signaling has catastrophic consequences for the developing embryo and it is now well appreciated that defective Wnt signaling is a causative factor for a number of pleiotropic human pathologies, including cancer. Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. The Notch signaling pathway is a highly conserved cell signaling system present in most animals. It plays an important role in cell-cell communication, and further regulates embryonic development.

MCE designs a unique collection of 349 Wnt/Hedgehog/Notch signaling pathway-related small molecules. Wnt/Hedgehog/Notch Compound Library serves as a useful tool for stem cell research and anti-cancer drug screening.

HY-L109

Protein-protein Interaction Inhibitor Library	576 compounds
Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs. However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures. With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 576 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.

Protein-protein Interaction Inhibitor Library

576 compounds

Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs.

However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures.

With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 576 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.

MUC1, mucin core	Mucin	Cancer
MUC1, mucin core is the region of the MUC1 mucin core. MUC1 is a type I transmembrane glycoprotein, and is overexpressed and aberrantly glycosylated in carcinoma cells. MUC1, mucin core protein binds to domain 1 of ICAM-1 .

IMAB027 ASP1650	Inhibitory Antibodies	Cancer
IMAB027 (ASP1650) is a specific anti-CLDN6 mAb, while CLDN6 (Claudin 6) is a tight junction membrane protein, aberrantly expressed in various human cancer types, ovarian cancers particularly. IMAB 027 shows anti-tumor activity, and induces apoptosis in CLDN6 ⁺ ovarian and testicular cancer cell lines .

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