Name | GNF-2 |
Description | GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl. |
Cell Research | Cells (0.3-0.6 × 106 per mL) are plated in duplicate or triplicate in 96-well plates containing increasing GNF-2 concentrations (5 nM–10 μM). After incubation at 37 ℃ in 5% CO2 for 48 hours, the effect of GNF-2 on cell viability is determined by the MTT colorimetric dye reduction method. Inhibition of cell proliferation is calculated as a percentage of growth of DMSO-treated cells, and IC50 values are determined with Microsoft Excel XLfit3.(Only for Reference) |
Kinase Assay | Binding assay: Recombinant proteins (100 nM for each construct) or immunoprecipitated proteins are diluted in kinase buffer (20 mM HEPES (pH 7.4), 50 mM KCl, 0.1% CHAPS, 30 mM MgCl2, 2 mM MnCl2, 1 mM DTT, and 1% glycerol). Aliquots of the diluted proteins are preincubated with either DMSO or compounds for 30 min at room temperature and then added to K-LISA PTK EAY reaction plates. The kinase reaction is initiated by adding 0.1 mM ATP and is allowed to proceed for 30 min at room temperature. The phosphorylation of GST-Abltide is monitored by SDS-PAGE and phosphorimaging analysis or autoradiography. |
In vivo | 1 μM GNF-2诱导 Ba/F3.p210 细胞和Ba/F3.p210E255V 细胞的凋亡。GNF-2以剂量依赖性方式抑制Bcr-abl的细胞酪氨酸磷酸化,IC5??0为267 nM。1 μM GNF-2诱导Ba/F3.p210细胞中磷酸化Stat5水平的显著降低。10 μM GNF-2需要BCR和/或 c-Abl SH3 和/或 SH2 域抑制BCR-Abl依赖性细胞增殖。10 μM GNF-2以剂量依赖性方式明显抑制CrkII的酪氨酸磷酸化。GNF-2作用于表达 c-AblG2A 的细胞,抑制CrkII 磷酸化,IC50为 0.051 μM。GNF-2抑制表达p210Bcr-Abl和p210Bcr-Abl突变体的BafF3细胞的自体磷酸化和增殖。与GNF-5(20 nM)组合的GNF-2(8 nM)在抑制Abl64-515激酶活性方面产生累加效应。GNF-2抑制Bcr-abl阳性细胞生长,IC50值为273 nM (K562) 和 268 nM (SUP-B15),这种作用具有剂量依赖性。GNF-2抑制Ba/F3.p210E255V Ba/F3.p185Y253H细胞生长,IC50分别为268 nM和194 nM。 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 37.4 mg/mL (100 mM) Ethanol : 18.7 mg/mL (50 mM)
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Keywords | SARS coronavirus | allosteric | non-ATP competitive inhibitor | Ba/F3.p185Y253H | Bcr-Abl | Ba/F3.p210E255V | GNF-2 | SARS-CoV | Ba/F3.p210 | bone erosion | Inhibitor | GNF 2 | inhibit |
Inhibitors Related | Umifenovir hydrochloride | Imatinib | Chloroquine phosphate | Andrographolide | Hydroxychloroquine | EIDD-1931 | Chloroquine | Silymarin | Ritonavir | Nirmatrelvir | Favipiravir | Remdesivir |
Related Compound Libraries | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Fluorochemical Library | Highly Selective Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | NO PAINS Compound Library | Anti-Viral Compound Library | Tyrosine Kinase Inhibitor Library |