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Results for "

NanoBRET

" in MedChemExpress (MCE) Product Catalog:

17

Inhibitors & Agonists

1

Fluorescent Dye

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145899
    PKN1/2-IN-1
    1 Publications Verification

    		 PKC Cancer
    PKN1/2-IN-1 is a potent cell permeabilizer and selective PKN1/2 inhibitor with IC50 values of 16 nM and 210 nM for PKN1 and PKN2, respectively, and Ki values of 8 nM and 108 nM, respectively. PKN1/2-IN-1 exhibits strong intracellular PKN2 binding capacity in NanoBRET assays (IC50 = 2.1 μM). PKN1/2-IN-1 can be used to study physiological processes such as tumor cell migration .
    PKN1/2-IN-1
  • HY-139004
    SGC-CK2-1
    5 Publications Verification

    		 Casein Kinase Neurological Disease
    SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases .
    SGC-CK2-1
  • HY-127104
    FMF-04-159-2
    4 Publications Verification

    AKOS-04

    		 CDK Cancer
    FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively .
    FMF-04-159-2
  • HY-178129
    MRL-SYKi

    		Syk Inflammation/Immunology
    MRL-SYKi is a chemical probe for gain-of-function variants of spleen tyrosine kinase (SYK). MRL-SYKi reduces the catalytic activity of SYK S550Y, SYK S550F and SYK P342T, and downregulates the phosphorylation level of SYK S550Y. MRL-SYKi serves as a template for developing NanoBRET tracers targeting SYK, enabling NanoBRET cellular target engagement assays for gain-of-function variants of SYK. MRL-SYKi is applicable to research related to inflammatory and immune diseases .
    MRL-SYKi
  • HY-153521
    CCT374705

    		BCL6 Cancer
    CCT374705 is an orally active BCL6 inhibitor (IC50 = 4.8 nM) with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
    CCT374705
  • HY-162266
    C3TD879

    		Ser/Thr Protease Cancer
    C3TD879 is a Type I kinase inhibitor that potently inhibits CITK catalytic activity (IC50 = 12 nM). C3TD879 binds directly to full-length human CITK in cells (NanoBRET Kd < 10 nM). C3TD879 is a chemical probe suitable for interrogating the complex biology of CITK .
    C3TD879
  • HY-155874
    ZNL-05-044

    		CDK Cancer
    ZNL-05-044 is a CDK11 inhibitor with an IC50s of 0.23 μM and 0.27 μM against CDK11A and CDK11B, respectively (NanoBRET assay). ZNL-05-044 leads to G2/M cell cycle arrest and impairs RNA splicing .
    ZNL-05-044
  • HY-149006
    CK156

    		DAPK Inflammation/Immunology Cancer
    CK156, a chemical probe, is a highly selective death-associated protein kinase (DAPK) inhibitor with IC50s of 182 nM,34 μM, and 39 μM in the DRAK1 NanoBRET assay for DRAK1, CK2a1, and CK2a2, respectively. CK156 can be used for the research of autoimmune and inflammatory diseases .
    CK156
  • HY-137115
    BODIPY-Cyclopamine

    		Smo Cancer
    BODIPY-Cyclopamine is a fluorescently labeled ligand for the Smoothened (SMO) receptor. The activation of SMO is regulated by Patch protein, and over-activated SMO signaling pathways are associated with tumorigenesis. The NanoBRET (Nanofluorescein bioluminescence resonance energy transfer) technique used in the study can sensitively detect the resonance energy transfer between SMO and BODIPY-Cyclopamine, which can be used for high-throughput screening and kinetic analysis. Studying the binding site of BODIPY-Cyclopamine on SMO can also further explore SMO-targeted drugs .
    BODIPY-Cyclopamine
  • HY-172118
    SGC-CDKL5/GSK3

    		GSK-3 Neurological Disease
    CDKL5/GSK3-IN-1 (Compound 2) is a potent and selectivity chemical probe for CDKL5/GSK3.CDKL5/GSK3-IN-1 has potent inhibition of CDKL5 and GSK3α/β, with IC50 values of 4.6, 24 and 9.5 nM for CDKL5, GSK3β and GSK3α, respectively, in the NanoBRET assay. CDKL5/GSK3-IN-1 can be used for the research of CNS diseases .
    SGC-CDKL5/GSK3
  • HY-175649
    LATS1/2-IN-1

    		Large Tumor Suppressor (LATS) YAP Cancer
    LATS1/2-IN-1 is a potent and selective LATS1 and LATS2 inhibitor. LATS1/2-IN-1 exhibits potent inhibitory activity against LATS1 and LATS2 with IC50 values of 4.4 nM and 5.5 nM as determined via r 33P functional assay. LATS1/2-IN-1 displays cellular IC50 values of 136 nM for LATS1 and 36.0 nM for LATS2 as determined via NanoBRET assay. LATS1/2-IN-1 reduces phosphorylation of YAP1 in mouse liver. LATS1/2-IN-1 demonstrates wound healing activity in HT-1080 scratch assay and in vivo SKH1 mouse punch biopsy model. LATS1/2-IN-1 can be used for the study of regenerative medicine indications such as wound healing .
    LATS1/2-IN-1
  • HY-175454
    YH-0623

    		DNA/RNA Synthesis PDGFR Oxidative Phosphorylation Mitochondrial Metabolism Cancer
    YH-0623 is an orally active mitochondrial RNA polymerase (POLRMT) inhibitor (IC50 = 50.48 nM, Nanoluciferase Bioluminescence Resonance Energy Transfer (NanoBRET) assay). YH-0623 exhibits antiproliferative effects on 22Rv1 cells by reducing the expression of mitochondrial-related genes. YH-0623 inhibits 22Rv1 cell growth, colony formation, and the expression of OXPHOS-related proteins. YH-0623 significantly inhibits tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research .
    YH-0623
  • HY-168908
    LIJTF500025

    		LIM Kinase (LIMK) Cancer
    LIJTF500025, a chemical probe, is a potent and selective LIMK inhibitor, with pIC50 values of 6.77 and 7.03 for LIMK1 and LIMK2, respectively, as determined by NanoBRET. LIJTF500025 can be used for the research of cancer .
    LIJTF500025
  • HY-151382
    CK2-IN-3

    		Casein Kinase Cancer
    CK2-IN-3 is a selective and potent CK2 inhibitor (Kd: 12 nM), with IC50 values of 1.51 μM (CK2α) and 7.64 μM (CK2α’). CK2-IN-3 can be used in the research of cancers .
    CK2-IN-3
  • HY-D2201
    Fluorescent ACKR3 antagonist 1

    		Fluorescent Dye Cancer
    Fluorescent ACKR3 antagonist 1(compound 18a) is a atypical chemokine receptor 3 antagonist .
    Fluorescent ACKR3 antagonist 1
  • HY-178974
    STK10-IN-1

    		Ser/Thr Kinase Cancer
    SLK/STK10-IN-2 (Compound 23) is a highly selective STK10 inhibitor, with a Kd of 365 nM and an IC50 of 0.85 μM. SLK/STK10-IN-2 exhibits EC50 of 0.89 μM in NanoBRET cell experiments. SLK/STK10-IN-2 shows no significant binding to SLK, STK3/4. SLK/STK10-IN-2 can be used to study STK10-related diseases (such as abnormal lymphocyte migration) .
    STK10-IN-1
  • HY-181004
    PKMYT1-IN-13

    		CDK Cancer
    PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer .
    PKMYT1-IN-13

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