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Results for "

nci-h358

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    11
    TargetMol | Inhibitors_Agonists
  • PROTAC Products
    1
    TargetMol | PROTAC
Alisertib
MLN 8237
T22411028486-01-2
Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.
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telaglenastat
CB-839, CB839, CB 839
T67971439399-58-2
Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.
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NVP 231
T1933362003-83-6
NVP-231 is a potent, specific and reversible CerK inhibitor(IC50=12±2 nM) that competitively inhibits ceramide binding to CerK.
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TargetMol | Inhibitor Sale
KRASG12C IN-14
T200204
KRASG12C IN-14 (compound 15), a potent inhibitor specifically designed for the KRAS G12C mutation, exhibits impressive efficacy in impeding CYPA-dependent KRAS-BRAF interaction and ERK phosphorylation in NCI-H358 cells, both with an IC 50 of 0.002 μM.
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KRAS G12D inhibitor 25
T2010062768099-61-0
KRAS G12D inhibitor 25 (Compound 148) acts as an inhibitor for KRAS G12C and HSP90α, displaying IC50 values of <0.1 μM and 0.1-1 μM respectively. Additionally, it suppresses the proliferation of MIA PaCa-2 and NCI-H358 cell lines, with EC50 values of <0.1 μM and 0.1-1 μM correspondingly. This compound also promotes the degradation of ERBB2, exhibiting a DC50 of 0.1-1 μM.
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KRAS G12C inhibitor 69
T204874
KRAS G12C inhibitor 69 (Compound K09) is an inhibitor of the mutant RAS protein KRAS G12C with an IC50 of 4.36 nM. In the cell lines NCI-H358 and MIA-PACA-2, it suppresses ERK phosphorylation with IC50 values of 12 nM and 7 nM, respectively. Additionally, KRAS G12C inhibitor 69 hinders the proliferation of NCI-H358 and MIA-PACA-2 cancer cells, with IC50 values of 3.15 nM and 2.33 nM, respectively.
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k20
T63823
K20 is a potent and selective inhibitor of KRas G12C (IC50: 1.16 nM). In H358 cells, K20 demonstrates an anticancer effect with an IC50 value of 0.78 μM and inhibits the growth of NCI-H358 tumor cells (TGI: 41%) without significant toxicity. K20 reduces the phosphorylation level of Erk, leading to apoptosis.
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10-14 weeks
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BI-0474
T695292750570-55-7
BI-0474 is a potent KRASG12C inhibitor that inhibits GDP-KRAS::SOS1 protein-protein interactions with an IC50 value of 7.0 nM.BI-0474 exhibits significant antiproliferative activity against NCI-H358 cells harboring the G12C mutation, and shows significant anti-tumor activity in a non-small cell lung cancer xenograft model. activity.BI-0474 can be used for cancer research.
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8-10 weeks
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SHP2-IN-14
T791082673400-91-2
SHP2-IN-14 (compound 27) is a potent, orally active allosteric inhibitor of SHP2 with an IC50 of 7 nM, exhibiting strong anti-tumor activity, inhibiting tumor progression in NCI-H358 tumor-bearing mice, and demonstrating favorable pharmacokinetic properties and safety [1].
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8-10 weeks
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HP661
T83865
HP661, a selective inhibitor of mitochondrial complex I (NADH dehydrogenase), impedes complex I activity by 77.6% at 1 µM, demonstrating lesser inhibition towards complex III (28.1%) and no inhibitory effects on complexes II and IV. It notably decreases the viability of human lung cancer cells—H460, NCI H441, and trametinib-resistant A549 cells (IC50s = 10.6, 29.7, and 15.1 nM, respectively)—which exhibit high levels of oxidative phosphorylation. In contrast, it shows minimal activity against NCI H358 lung cancer cells and non-cancerous HPNE and MRC-5 cells (IC50s = >10,000 nM for both), which have lower oxidative phosphorylation levels. Furthermore, in an H460 mouse xenograft model, HP661 at a dose of 30 mg/kg twice daily significantly reduces tumor volume and enhances the tumor-growth inhibitory effects of trametinib.
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PROTAC SOS1 degrader-5
T872682836273-61-9
PROTAC SOS1 degrader-5 (compound 4) serves as an effective degrader of PROTAC SOS1, exhibiting a DC50 of 13 nM. It robustly suppresses the proliferation of NCI-H358 cells, with an IC50 value of 5 nM [1].
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