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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
21 Results for "
GNE cells
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "GNE cells" in MCE Product Catalog:
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9 Publications Verification
Research Areas:
GNE-140 racemate is a racemic mixture of (R)-GNE-140 (HY-100742A) and (S)-GNE-140 (HY-100742B), and also a tautomer of GNE-140 (HY-118241). GNE-140 racemate is an orally active lactate dehydrogenase inhibitor, with an IC50 of 3 nM against human LDHA and an IC50 of 5 nM against LDHB. GNE-140 racemate reduces the phosphorylation level and total protein expression of p38 MAPK, and inhibits EGF-induced AKT phosphorylation. GNE-140 racemate decreases lactate production, regulates glycolysis, the pentose phosphate pathway and nucleotide biosynthesis, increases extracellular pH, inhibits cell proliferation, migration and invasion, and induces caspase-3 activation and ROS accumulation. GNE-140 racemate can be used in research related to breast cancer, cystic fibrosis and pancreatic cancer .
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7 Cited Publications
GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
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2 Cited Publications
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 .
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1 Cited Publications
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GNE-987 is a VHL-dependent BRD4 PROTAC degrader. 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 can be used for the research of cancer .
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1 Cited Publications
Cat. No.: HY-19775
CAS No.: 1677668-27-7
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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 .
Cat. No.: HY-158113
CAS No.: 3037549-86-0
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CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
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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 .
Cat. No.: HY-19774
CAS No.: 1677667-24-1
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GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell.
Cat. No.: HY-160821A
CAS No.: 335275-62-2
Synonyms: ManNAc-6P sodium salt
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N-Acetylmannosamine 6-phosphate sodium salt is a NanR modulator and an intermediate in the sialic acid pathway. N-Acetylmannosamine 6-phosphate sodium salt disrupts the binding of NanR to the promoter regions of nanAT and nanE, and prevents NanR-mediated transcriptional repression of these loci. N-Acetylmannosamine 6-phosphate sodium salt acts as a key precursor for sialic acid biosynthesis, participating in this process via Neu5Ac-9-P synthase. N-Acetylmannosamine 6-phosphate sodium salt can be used in research related to GNE myopathy .
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GNE-6893 is an orally active, selective HPK1 inhibitor with a Ki < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers .
Cat. No.: HY-16984
CAS No.: 1705602-02-3
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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 .
Cat. No.: HY-174261
CAS No.: 3082412-00-5
KRAS-IN-5 (Compound Ex 6) is an orally active and selective inhibitor targeting KRAS mutants (including KRAS G12D, KRAS G12V, KRAS WT) with a GNE IC50 value of 1.3 nM against KRAS G12D. KRAS-IN-5 blocks tumor cell proliferation by inhibiting KRAS-mediated signaling pathways (e.g., reducing ERK phosphorylation). KRAS-IN-5 is promising for research of KRAS mutation-related cancers, such as pancreatic cancer, colorectal cancer, lung cancer .
Cat. No.: HY-15882
CAS No.: 1200127-66-7
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GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
Cat. No.: HY-13847
CAS No.: 1428902-71-9
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 .
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GNE-274 is a non-degrading estrogen receptor α (ERα/ESR1) modulator structurally similar to GDC-0927 (HY-111484). GNE-274 competes for binding to the ligand-binding domain of ERα and induces a coregulator-binding conformation similar to that of antagonists, yet retains partial agonistic transcriptional activity and does not promote ERα turnover. GNE-274 effectively inhibits E2-stimulated proliferation of ER-positive, HER2-negative breast cancer cells. GNE-274 promotes the recruitment of ERα to the nucleus and chromatin, increases chromatin accessibility, while largely maintaining the intranuclear mobility of ERα. GNE-274 can be used in research on ER-positive breast cancer and ERα transcriptional dynamics .
Cat. No.: HY-129937
CAS No.: 2738533-33-8
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(S)-GNE-987 is an isomer of GNE-987 (HY-129937A), which loses VHL binding capacity and BRD4 protein degradation activity, but retains BRD4 inhibitory activity. (S)-GNE-987 is a BRD4/BET inhibitor that potently binds to the BD1 and BD2 bromodomains of BRD4, with a BRD4 BD1 IC50 of 4.0 nM and a BRD4 BD2 IC50 of 3.9 nM. (S)-GNE-987 inhibits MYC expression and exhibits inhibitory activity against acute myeloid leukemia cells, whereas its CLL1‑6 antibody-drug conjugate shows almost no in vivo antitumor efficacy in the HL‑60 xenograft tumor model. (S)-GNE-987 can be used in related research on acute myeloid leukemia .
Cat. No.: HY-175445
CAS No.: 2417369-99-2
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GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer .
Cat. No.: HY-189477
CAS No.: 1557236-81-3
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GNE-7056 is an orally active interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.2 nM against human kinase, and exhibits high selectivity over LCK kinase. GNE-7056 inhibits PLCγ-1 phosphorylation, suppresses the production of IL-2, IL-4, IL-13 and TH2 cytokines, reduces CD4 + T-cell proliferation, and inhibits activation-induced cell death of CD4 + T cells by decreasing the abundance of FasL. GNE-7056 can be used in asthma-related research .
Cat. No.: HY-100742R
CAS No.: 1802977-61-2
GNE-140 racemate (Standard) is the analytical standard of GNE-140 racemate (HY-100742). This product is intended for research and analytical applications. GNE-140 racemate is a racemic mixture of (R)-GNE-140 (HY-100742A) and (S)-GNE-140 (HY-100742B), and also a tautomer of GNE-140 (HY-118241). GNE-140 racemate is an orally active lactate dehydrogenase inhibitor, with an IC50 of 3 nM against human LDHA and an IC50 of 5 nM against LDHB. GNE-140 racemate reduces the phosphorylation level and total protein expression of p38 MAPK, and inhibits EGF-induced AKT phosphorylation. GNE-140 racemate decreases lactate production, regulates glycolysis, the pentose phosphate pathway and nucleotide biosynthesis, increases extracellular pH, inhibits cell proliferation, migration and invasion, and induces caspase-3 activation and ROS accumulation. GNE-140 racemate can be used in research related to breast cancer, cystic fibrosis and pancreatic cancer .
Cat. No.: HY-187181
CAS No.: 2933893-78-6
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GNE-2181 is an orally active, blood-brain barrier-penetrant pan-TEAD transcription factor inhibitor, with IC50 values of 13, 26, 61 and 17 nM against TEAD1, TEAD2, TEAD3 and TEAD4, respectively. GNE-8021 allosterically disrupts the TEAD-YAP/TAZ interaction and inhibits TEAD-mediated oncogenic transcriptional programs via the Hippo signaling pathway. GNE-8021 suppresses YAP-driven tumor cell growth. GNE-2181 inhibits the growth of intracranial tumor models in vivo. GNE-2181 can be used for research on brain metastasis of lung cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
