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Results for "

isoform specificity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5 alpha Reductase (2) Apoptosis (2) Aurora Kinase (1) Complement System (1) Cytochrome P450 (1) DNA Methyltransferase (1) Endogenous Metabolite (1) FGFR (1) Fluorescent Dye (1) HDAC (2) PDHK (1) PI3K (1) PPAR (1) PROTACs (1) Proteasome (1) Reference Standards (1) YAP (1)
By Research Areas:	Cancer (7) Inflammation/Immunology (1) Metabolic Disease (3) Neurological Disease (1)

Inhibitors & Agonists

Fluorescent Dye

Natural
Products

Targets Recommended: DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-163705

BR-cpd7	PROTACs FGFR	Cancer
BR-cpd7 is a PROTAC degrader for fibroblast growth factor receptor FGFR1/2 with DC₅₀ of 10 nM. BR-cpd7 arrests cell cycle, inhibits proliferations of FGFR1/2 aberrant activated tumor cells. (Pink: ligand for target protein FGFR-IN-12 (HY-160013); Black: linker; Blue: ligand for E3 ligase Thalidomide-NH-CH2-COOH (HY-131717))

HY-110136A

PMX 205 Trifluoroacetate Maximum Cited Publications 8 Publications Verification	Complement System	Inflammation/Immunology
PMX 205 Trifluoroacetate is a specific complement C5aR1 isoform antagonist .

HY-114702

M77976 1 Publications Verification	PDHK	Metabolic Disease
M77976 is a specific ATP-competitive inhibitor of *PDK4 (pyruvate dehydrogenase kinase isoforms* 4), with an IC₅₀** of 648 μM. M77976 is potential for the research of obesity and diabetes .

HY-155338

SWTX-143	YAP	Cancer
SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .

HY-107385

Epristeride 1 Publications Verification ONO-9302; SKF105657	5 alpha Reductase	Cancer
Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of *human steroid 5 alpha-reductase isoform* 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with K_i** value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .

HY-145155

Calpain-2-IN-1 2 Publications Verification	Proteasome	Neurological Disease
Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with K_is of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function .

HY-116862

Dibenzylfluorescein DBF	Cytochrome P450 Fluorescent Dye	Others
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its K_m value of 0.87-1.9 μM (Ex=485 nm，Em=535 nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .

HY-107385R

Epristeride (Standard) ONO-9302 (Standard); SKF105657 (Standard)	Reference Standards 5 alpha Reductase	Cancer
Epristeride (Standard) is the analytical standard of Epristeride. This product is intended for research and analytical applications. Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of *human steroid 5 alpha-reductase isoform* 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with K_i** value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .

HY-121998

Binucleine 2	Aurora Kinase	Others
Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.

HY-168088

DNMT1/HDAC-IN-1	HDAC DNA Methyltransferase	Cancer
DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC₅₀=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .

HY-172159

FF2039	HDAC Apoptosis	Cancer
FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC₅₀s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC₅₀s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .

HY-111355B

Cholesteryl sulfate sodium	Endogenous Metabolite	Metabolic Disease
Cholesteryl sulfate sodium is an orally available, NPC2-targeted cholesterol biosynthesis agonist. Cholesteryl sulfate sodium activates SREBP2 by competitively binding to NPC2, promoting cholesterol synthesis (EC₅₀=50 μM). Cholesteryl sulfate sodium enhances the self-assembly ability of Mitoxantrone hydrochloride (HY-13502A), while repairing the intestinal mucosal barrier and inhibiting inflammation by regulating serine protease activity and PKCη signaling pathway. Cholesteryl sulfate sodium is a component of the platelet cell membrane and supports platelet adhesion. Cholesteryl sulfate sodium also regulates the activity of selective protein kinase C isoforms and modulates the specificity of PI3K, playing a role in keratinocyte differentiation .

HY-126969

C333H	PPAR	Metabolic Disease
C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .

HY-12491

PIK-C98	PI3K Apoptosis	Cancer
PIK-C98 is a potent and selective PI3K inhibitor, with IC₅₀s of 0.59, 1.64, 3.65, and 0.74 μM for α, β, δ, and γ isoforms, respectively. PIK-C98 inhibits all class I PI3Ks but has no effects on AKT or mTOR activity. PIK-C98 interferes with the ATP-binding pockets of PI3Ks by forming H-bonds and arene-H interactions with specific amino acid residues. PIK-C98 induces apoptosis by inhibiting PI3K. PIK-C98 can be used for the research of multiple myeloma .

Cat. No.	Product Name	Type

HY-116862

Dibenzylfluorescein DBF	Fluorescent Dyes/Probes
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its K_m value of 0.87-1.9 μM (Ex=485 nm，Em=535 nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .

Dibenzylfluorescein

DBF

Fluorescent Dyes/Probes

Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its K_m value of 0.87-1.9 μM (Ex=485 nm，Em=535 nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-111355B

Cholesteryl sulfate sodium	Structural Classification Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields Steroids	Endogenous Metabolite
Cholesteryl sulfate sodium is an orally available, NPC2-targeted cholesterol biosynthesis agonist. Cholesteryl sulfate sodium activates SREBP2 by competitively binding to NPC2, promoting cholesterol synthesis (EC₅₀=50 μM). Cholesteryl sulfate sodium enhances the self-assembly ability of Mitoxantrone hydrochloride (HY-13502A), while repairing the intestinal mucosal barrier and inhibiting inflammation by regulating serine protease activity and PKCη signaling pathway. Cholesteryl sulfate sodium is a component of the platelet cell membrane and supports platelet adhesion. Cholesteryl sulfate sodium also regulates the activity of selective protein kinase C isoforms and modulates the specificity of PI3K, playing a role in keratinocyte differentiation .

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