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Phenotyping Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Acyltransferase (1) ADC Cytotoxin (1) Akt (3) Amyloid-β (1) Androgen Receptor (1) Apoptosis (4) c-Fms (1) Epigenetic Reader Domain (1) FLAP (1) GCGR (1) HDAC (1) Histone Demethylase (1) HIV Integrase (1) HPV (1) ICMT (1) IGF-1R (1) JNK (1) Kinesin (1) MEK (1) Microtubule/Tubulin (1) Mitochondrial Metabolism (1) MMP (1) P-glycoprotein (1) PDHK (1) PI3K (1) SHP2 (1) Src (1) Topoisomerase (1)
By Research Areas:	Cancer (14) Infection (1) Inflammation/Immunology (5) Metabolic Disease (2) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0790

Lupeol 3 Publications Verification Clerodol; Monogynol B; Fagarasterol	Androgen Receptor Apoptosis	Cancer
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

HY-120766

NCDM-32B

Histone Demethylase Cancer

NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer .

NCDM-32B	Histone Demethylase	Cancer
NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer .

HY-Y0586

2,4,5-Trimethoxybenzoic acid
2,4,5-Trimethoxybenzoic acid is a compound identified in purple perilla extracts. 2,4,5-Trimethoxybenzoic acid inhibits M1 macrophage phenotype-mediated inflammation in diabetes .

HY-117651

2-Fluoropalmitic acid	Acyltransferase	Cancer
2-Fluoropalmitic acid, an acyl-CoA synthetase inhibitor, acts as a candidate anti-glioma agent. 2-Fluoropalmitic acid suppresses the viability and stem-like phenotype of glioma stem cells (GSCs). 2-Fluoropalmitic acid also inhibits proliferation and invasion of glioma cell lines .

HY-149711

Farnesylcysteine	ICMT	Metabolic Disease
Farnesylcysteine (FC) is a competitive inhibitor of ICMT. The fcly mutant has quantitatively low farnesylcysteine (FC) lyase activity and an enhanced response to ABA. Farnesylcysteine induces an ABA hypersensitive phenotype in Arabidopsis thaliana .

HY-145110

IGF-1R inhibitor-2	IGF-1R	Cancer
IGF-1R inhibitor-2 (example 121) is an insulin-like growth factor-1 receptor (IGF-1R) inhibitor. Downregulation of IGF-1R can reverse the transformed phenotype of tumor cells and potentially render them susceptible to apoptosis .

HY-125331

DRF-1042	Topoisomerase ADC Cytotoxin	Cancer
DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype .

HY-156109

PDK-IN-2	PDHK Mitochondrial Metabolism	Cancer
PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC₅₀: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .

HY-P0119

Lixisenatide 1 Publications Verification	GCGR MEK Akt MMP JNK	Neurological Disease Metabolic Disease Inflammation/Immunology
Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe ^−/− Irs ^2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation .

HY-N0284

Esculetin 3 Publications Verification	PI3K Akt	Inflammation/Immunology Cancer
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .

HY-13224

AZD4877	Kinesin Apoptosis	Cancer
AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC₅₀ of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity .

HY-150565

P-gp inhibitor 5	P-glycoprotein	Cancer
P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In ^TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015) .

HY-18620

DZ2002 1 Publications Verification	Others	Inflammation/Immunology
DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (K_i=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis .

HY-137892

GSK620	Epigenetic Reader Domain	Inflammation/Immunology
GSK620 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-123298

Chrysotoxine	Src Akt Apoptosis	Cancer
Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research .

HY-101855

Emrusolmin Anle138b	Amyloid-β	Neurological Disease
Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .

HY-Y0493

HODHBt HOOBt
HODHBt (HOOBt) inhibits STAT5-SUMO interaction by blocking SUMOylation of phosphorylated STAT5. HODHBt enhances the magnitude of IL-15 signaling and significantly increases the natural killer (NK) cell cytotoxicity phenotype and function and the generation of cytokine-induced memory-like (CIML) natural killer (NK) cells. HODHBt can be used for research of HIV-infection and cancer .

HY-100384

NKL 22 1 Publications Verification	HDAC	Neurological Disease
NKL 22 (compound 4b) is a potent and selective inhibitor of histone deacetylases (HDAC), with an IC₅₀ of 199 and 69 nM for HDAC1 and HDAC3, respectively. NKL 22 exhibits selectivity over HDAC2/4/5/7/8 (IC₅₀≥1.59 μM). NKL 22 ameliorates the disease phenotype and transcriptional abnormalities in Huntington's disease transgenic mice .

HY-152208

BPDA2	SHP2	Cancer
BPDA2 is a highly selective and competitive active site SHP2 inhibitor with IC₅₀s of 92.0 nM, 33.39 μM, 40.71 μM for SHP2, SHP1, SHP1B, respectively. DBDA2 downregulates mitogenic and cell survival signaling and RTK expression. BPDA2 suppresses SHP2 mediated signaling and breast cancer cell phenotypes .

HY-144256

CHD1Li 6.11	Others	Cancer
CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC₅₀=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties .

HY-120599

Sabizabulin 2 Publications Verification VERU-111; ABI-231	Microtubule/Tubulin Apoptosis HPV	Cancer
VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC₅₀ of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer .

HY-N6711

Equisetin	HIV Integrase	Infection
Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537 . Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity . Equisetin inhibits the growth of Gram-positive bacteria and HIV-1 integrase activity but shows no activity against Gram-negative bacteria . Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections .

HY-139990

CSF1R-IN-3	c-Fms	Cancer
CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC₅₀=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity .

HY-155408

ALR-27	FLAP	Inflammation/Immunology
ALR-27 is an antagonist of the 5-lipoxygenase (5-LOX) activating protein FLAP and has anti-inflammatory activity. ALR-27 potently inhibits 5-LOX product formation (>80%) in pro-inflammatory M1-MDM, with no significant direct inhibition of 5-LOX. ALR-27 not only reduces prostaglandin and leukotriene (LT) production in neutrophils but also increases the production of specialized prolytic mediators in specific human macrophage phenotypes .

Highly Selective Inhibitors Library	4643 compounds
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 4643 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes

Lixisenatide 1 Publications Verification	GCGR MEK Akt MMP JNK	Neurological Disease Metabolic Disease Inflammation/Immunology
Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe ^−/− Irs ^2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation .

Lupeol 3 Publications Verification Clerodol; Monogynol B; Fagarasterol	Triterpenes Structural Classification other families Classification of Application Fields Terpenoids Source classification Plants Disease Research Fields Cancer	Androgen Receptor Apoptosis
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

Esculetin 3 Publications Verification	Structural Classification Classification of Application Fields Oleaceae Source classification Fraxinus rhynchophylla Hance Coumarins Phenols Polyphenols Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields	PI3K Akt
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .

Equisetin	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics	HIV Integrase
Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537 . Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity . Equisetin inhibits the growth of Gram-positive bacteria and HIV-1 integrase activity but shows no activity against Gram-negative bacteria . Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections .

Chrysotoxine	Structural Classification Monophenols Orchidaceae Source classification Phenols Plants Dendrobium pulchellum Roxb. et Lindl. :Lindl.	Src Akt Apoptosis
Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research .

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Phenotyping Inhibitors

Inhibitors & Agonists

Screening Libraries

Peptides

NaturalProducts

Natural
Products