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Results for "

isoform-selective

" in MedChemExpress (MCE) Product Catalog:

19

Inhibitors & Agonists

2

Peptides

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108532
    AC-261066

    		RAR/RXR Cancer
    AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0 .
    AC-261066
  • HY-16596
    CNX-1351

    		PI3K Cancer
    CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
    CNX-1351
  • HY-108526
    AC-55649

    		RAR/RXR Autophagy Others
    AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
    AC-55649
  • HY-134194
    KL201
    1 Publications Verification

    		 Cryptochrome Metabolic Disease
    KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues .
    KL201
  • HY-123825
    GX-674

    		Sodium Channel Cardiovascular Disease Neurological Disease
    GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 of 0.1 nM at -40 mV .
    GX-674
  • HY-125838
    J30-8

    		JNK Neurological Disease
    J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases .
    J30-8
  • HY-P2261
    STAD 2

    		PKA Infection
    STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .
    STAD 2
  • HY-153450
    JBI-589

    		Protein Arginine Deiminase Cancer
    JBI-589 is a non-covalent PAD4 isoform-selective inhibitor. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors .
    JBI-589
  • HY-D1341
    Coumberone

    		Fluorescent Dye Cancer
    Coumberone is a metabolic fluorogenic probe, and isoform-selective substrate for all AKR1C isoforms. Coumberone can be reduced by all four members of the AKR1C family to its fluorescent alcohol coumberol. Coumberone can be used for the research of AKR1C .
    Coumberone
  • HY-131305
    HBDDE

    		PKC Apoptosis Neurological Disease
    HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis .
    HBDDE
  • HY-128772
    XPC-6444

    		Sodium Channel Neurological Disease
    XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity .
    XPC-6444
  • HY-137295
    Ingenol 3,20-dibenzoate

    		PKC Apoptosis Inflammation/Immunology
    Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells .
    Ingenol 3,20-dibenzoate
  • HY-18540
    KT109

    		MAGL Metabolic Disease Inflammation/Immunology
    KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC50=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-arachidonoylglycerol (2-AG), arachidonic acid and eicosanoids in mouse peritoneal macrophages .
    KT109
  • HY-119254
    BAY-850
    4 Publications Verification

    		 Epigenetic Reader Domain Metabolic Disease
    BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC50 of 166 nM.
    BAY-850
  • HY-112286
    PI3Kγ inhibitor 2

    		PI3K Inflammation/Immunology
    PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM .
    PI3Kγ inhibitor 2
  • HY-155671
    HDAC6-IN-18

    		HDAC Cancer
    HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6 isoform selective inhibitor with potent anti-multiple myeloma activity. HDAC6-IN-18 has HDAC6 inhibitory activity in RPMI8266, U266 and MM.1S cells with IC50 values of 0.17, 0.7 and 0.42 μM, respectively .
    HDAC6-IN-18
  • HY-111509
    TAK-828F

    		ROR Inflammation/Immunology
    TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ) .
    TAK-828F
  • HY-13531
    AS-604850
    1 Publications Verification

    		 PI3K Cancer
    AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
    AS-604850
  • HY-P5740
    Cacaoidin

    		Bacterial Infection
    Cacaoidin is a glycosylated lantibiotic isolated from a Streptomyces cacaoi strain. Cacaoidin has potent antibacterial activity against Gram-positive pathogens including Clostridium difficile .
    Cacaoidin

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