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Results for "

GNE

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71

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100742
    GNE-140 racemate
    5 Publications Verification

    		 Lactate Dehydrogenase Cancer
    GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor .
    <em>GNE</em>-140 racemate
  • HY-12410
    GNE-9822

    		Itk Inflammation/Immunology
    GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma .
    <em>GNE</em>-9822
  • HY-149056
    GNE-6893

    		MAP4K Cancer
    GNE-6893 is a potent and orally active HPK1 inhibitor. GNE-6893 can be used in research of cancer .
    <em>GNE</em>-6893
  • HY-145341
    GNE-149

    		Estrogen Receptor/ERR Cancer
    GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
    <em>GNE</em>-149
  • HY-U00428
    GNE 220

    		MAP4K Cancer
    GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC50 of 7 nM.
    <em>GNE</em> 220
  • HY-12517
    GNE-293

    		PI3K Inflammation/Immunology
    GNE-293 is a potent and selective PI3Kδ inhibitor (IC50 = 4.38 nM). GNE-293 has favorable pharmacokinetic properties. GNE-293 can be used for research of asthma, rheumatoid arthritis, and other inflammatory disorders .
    <em>GNE</em>-293
  • HY-142160
    GNE-9815

    		Raf Cancer
    GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
    <em>GNE</em>-9815
  • HY-132294
    GNE-502

    		Estrogen Receptor/ERR Cancer
    GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer .
    <em>GNE</em>-502
  • HY-141551
    GNE-274

    		Estrogen Receptor/ERR Cancer
    GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research .
    <em>GNE</em>-274
  • HY-123621
    GNE-375

    		Epigenetic Reader Domain Cancer
    GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin .
    <em>GNE</em>-375
  • HY-12282
    GNE-9605

    		LRRK2 Neurological Disease
    GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
    <em>GNE</em>-9605
  • HY-147214
    GNE-7883

    		YAP Cancer
    GNE-7883 is a pan-TEAD inhibitor with anti-cell proliferation activity. GNE-7883 overcomes resistance to KRAS G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation. GNE-7883 may be used in the study of YAP/TAZ-dependent cancers .
    <em>GNE</em>-7883
  • HY-107498
    GNE-8324

    		iGluR Neurological Disease
    GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons .
    <em>GNE</em>-8324
  • HY-129937A
    GNE-987

    		PROTACs Epigenetic Reader Domain Cancer
    GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .
    <em>GNE</em>-987
  • HY-150289
    GNE-235

    		Others Cancer
    GNE-235 is a compound selective for the second bromodomain of PBRM1, with a KD of 0.28 ± 0.02 μM. GNE-235 can be used for evaluation of the cellular function of PBRM1 .
    <em>GNE</em>-235
  • HY-108696
    GNE-781
    3 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .
    <em>GNE</em>-781
  • HY-12628
    GNE-618
    1 Publications Verification

    		 NAMPT Cancer
    GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity .
    <em>GNE</em>-618
  • HY-129527
    GNE-9278

    		iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity .
    <em>GNE</em>-9278
  • HY-15883
    GNE-900

    		Checkpoint Kinase (Chk) Apoptosis Cancer
    GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
    <em>GNE</em>-900
  • HY-19775
    GNE-6468

    		ROR Inflammation/Immunology
    GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC50 value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC50 of 30 nM for IL-17 PBMC .
    <em>GNE</em>-6468
  • HY-149026
    GNE-064

    		Epigenetic Reader Domain Others
    GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis .
    <em>GNE</em>-064
  • HY-12947
    GNE-3511
    5+ Cited Publications

    		 MAP3K Neurological Disease
    GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases .
    <em>GNE</em>-3511
  • HY-108435
    GNE-049
    3 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively .
    <em>GNE</em>-049
  • HY-16984
    GNE-4997

    		Itk Inflammation/Immunology
    GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity .
    <em>GNE</em>-4997
  • HY-107986
    GNE-6776
    3 Publications Verification

    		 Deubiquitinase Cancer
    GNE-6776 is a selective and orally bioavailable USP7 inhibitor .
    <em>GNE</em>-6776
  • HY-13847
    GNE-555

    		mTOR Cancer
    GNE-555 is a selective, metabolically stable mTOR inhibitor (Ki=1.5 nM) that also has good oral bioavailability. GNE-555 exhibits antiproliferative activity on PC3 and MCF-7 cells and can be used in cancer research .
    <em>GNE</em>-555
  • HY-123824
    GNE-0439

    		Sodium Channel Neurological Disease
    GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders .
    <em>GNE</em>-0439
  • HY-12632
    GNE 2861

    		PAK Cancer
    GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.
    <em>GNE</em> 2861
  • HY-18163
    GNE-7915
    5+ Cited Publications

    		 LRRK2 Neurological Disease
    GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
    <em>GNE</em>-7915
  • HY-18163A
    GNE-7915 tosylate
    5+ Cited Publications

    		 LRRK2 Neurological Disease
    GNE-7915 tosylate is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
    <em>GNE</em>-7915 tosylate
  • HY-114332
    GNE-8505

    		MAP3K Neurological Disease
    GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK) .
    <em>GNE</em>-8505
  • HY-100726
    GNE-272
    2 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300 .
    <em>GNE</em>-272
  • HY-100343
    GNE-495
    4 Publications Verification

    		 MAP4K Cancer
    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
    <em>GNE</em>-495
  • HY-120028
    GNE-207

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells .
    <em>GNE</em>-207
  • HY-117865
    GNE-886

    		Epigenetic Reader Domain Cancer
    GNE-886 (Compound 21) is a potent and selective inhibitor of Cat eye syndrome chromosome region candidate 2 bromodomain (CECR2) (BRD) with an IC50 value of 0.016 µM and an EC50 value of 370 nM. GNE-886 also inhibits BRD9 with an IC50 value of 1.6 µM .
    <em>GNE</em>-886
  • HY-112279
    GNE-131

    		Sodium Channel Neurological Disease
    GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
    <em>GNE</em>-131
  • HY-19774
    GNE-0946

    		ROR Inflammation/Immunology
    GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell.
    <em>GNE</em>-0946
  • HY-10812
    GNE-490

    		PI3K mTOR Cancer
    GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for  PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
    <em>GNE</em>-490
  • HY-15766
    GNE-617
    5+ Cited Publications

    		 NAMPT Metabolic Disease Cancer
    GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
    <em>GNE</em>-617
  • HY-15766A
    GNE-617 hydrochloride
    5+ Cited Publications

    		 NAMPT Cancer
    GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
    <em>GNE</em>-617 hydrochloride
  • HY-12763
    GNE-317
    1 Publications Verification

    		 PI3K mTOR Cancer
    GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).
    <em>GNE</em>-317
  • HY-11042
    GNE-477
    1 Publications Verification

    		 PI3K mTOR Cancer
    GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
    <em>GNE</em>-477
  • HY-U00428A
    GNE 220 hydrochloride

    		MAP4K Cancer
    GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
    <em>GNE</em> 220 hydrochloride
  • HY-15796
    GNE0877
    2 Publications Verification

    		 LRRK2 Neurological Disease
    GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC50 of 3 nM and a Ki of 0.7 nM. GNE0877 can be used for the research of neuroscience .
    <em>GNE</em>0877
  • HY-101783
    GNE-955

    		Pim Cancer
    GNE-955 is a potent and orally active pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.
    <em>GNE</em>-955
  • HY-108337
    GNE-0723

    		iGluR Neurological Disease
    GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively .
    <em>GNE</em>-0723
  • HY-126291
    GNE-616

    		Sodium Channel Neurological Disease
    GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively .
    <em>GNE</em>-616
  • HY-112803
    GNE-371

    		DNA/RNA Synthesis Cancer
    GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).
    <em>GNE</em>-371
  • HY-148238
    GNE-2256

    		IRAK Inflammation/Immunology
    GNE-2256 (molecule 19) is an orally active IRAK4 (Interleukin 1 receptor associated kinase 4) inhibitor (IRAK4 Ki=1.4 nM; IL-6 IC50=190 nM) .
    <em>GNE</em>-2256
  • HY-107423
    GNE 6901

    		iGluR Neurological Disease
    GNE 6901 (compound 40) is a potent GluN2A-selective NMDAR positive allosteric modulator (PAM) with an EC50 of 382 nM .
    <em>GNE</em> 6901

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