Perk ic50
GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. WebJul 22, 2024 · Compound 1 reduced pERK and pAKT levels in a dose-dependent manner in NCI-H358 cells, leading to an antiproliferative effect in NCI-H358 cells under nonadherent, low serum conditions. The effects of 1 were confirmed to be KRAS-driven and not off-target through the consistent data generated for the 10-fold less active distomer 44 and through …
Perk ic50
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WebGSK2656157 is a highly selective inhibitor of protein kinase R-like ER kinase (PERK) with IC50 value of 0.9nM [1]. GSK2656157 is highly selective for PERK enzyme against a panel … WebWe are the leading supplier of radiochemicals in a wide range of fields, from drug discovery to plant sciences.
WebBI-2852 inhibits RAS-mediated signaling and proliferation of KRAS-G12C-bearing NCI-H358 lung cancer cells (EGF-induced pERK IC50 = 5.8 μM; GI50 = 6.7 μM in soft agar with low serum) by blocking KRAS interactions with GEF SOS1 (GDP-bound G12C/G12D IC50 = 450/260 nM, GTP-bound Wt/G12C/G12D IC50 = 490/360/490 nM) and effectors CRAF … WebPERK inhibitor Product Citations (2) GSK2606414 Chemical Structure CAS NO. 1337531-36-8 GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 …
WebPERK Inhibitor I, GSK2606414, CAS 1337531-89-1, is a cell-permeable, highly potent EIF2AK3/PERK inhibitor (IC50 = 0.4 nM) that targets PERK in its inactive DFG conformation at the ATP-binding reg More>> MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents. SDS CoA References Data Sheet Webgenerate IC50 values, reported in nM. MRTX1257 was more potent in the 3D than the 2D format, as previously reported (Ref). C. MRTX1257 was added to KRAS G12C mutant (H358, MIA PaCa-2) or KRAS WT (H1299) cells for 3hrs (pERK) or 24hrs (pS6) over 9 point concentration response and reduction of effector signaling was
Webused to generate the PERK protein electrostatic environment in Flare, starting from PDB 4G31 and including the water molecule bridging the interaction between the carboxamide carbonyl and V952, V651. The protein interaction potentials for PERK nicely complement those of GSK6414. The electron-rich pyrrolo[2,3-d]pyrimidine heteroaryl system and the
WebThe IC50ratios for mutant to wild-type cells were higher than those for third-generation EGFR TKIs. Third-generation EGFR TKI osimertinib was highly potent against EGFR exon 20 … cheap smart carsWebAMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy. - … cyber security officer security clearanceWebThe IC50 was calculated using graphpad prism 6.0 (GraphPad Software, Inc., La Jolla, CA, USA). The `log (inhibitor) versus normalized response–Variable slope' equation was used … cyber security official websiteWebPERK inhibitor Product Citations (2) ISRIB Chemical Structure CAS NO. 1597403-47-8 ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM. Availability: In stock Free … cheap smart cardsWebpercs.DOC 4/25/2006 a) For uncompacted Class I and uncompacted Class II soils, the results of the particle size analysis, the soil type and the soil classification must be used … cheap smart cars londonWebgsk2606414是一种选择性的perk抑制剂，ic50值为0.4 nm[1]。 prkr样内质网激酶或蛋白激酶r（pkr）样内质网激酶（perk），也被称为真核翻译起始因子2-α激酶3（eif2ak3），属 … cheap smart car for saleWebA cell-permeable pyrrolopyrimidinamine compound that acts as a potent, ATP-competitive EIF2AK3/PERK inhibitor (IC 50 = 0.9 nM; [ATP] = 10 µM), displaying ≥511-fold selectivity over HRI/EIF2AK1, BRK, PKR/EIF2AK2, and MEKK2 (IC 50 = 460, 822, 905, and 954 nM, respectively) and much reduced or little activity toward more than 300 other kinases. cheap smart cars for sale