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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC74245 STK018404 STK018404 is a small molecule inhibitor of RNA-binding protein human antigen R (HuR), decreases the binding of HuR to its target RNA motif.
DC74246 AA132 AA132 (AA-132) is a small molecule activator of UPR signaling, covalently modifies a subset of ER protein disulfide isomerases (PDIs), activates global UPR signaling through a mechanism analogous to that of AA147.
DC74247 AG-946 Featured AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.
DC74248 HA344 HA344 (HA 344) is a dual covalent inhibitor of pyruvate kinase M2 (PKM2) and inosine monophosphate dehydrogenase (IMPDH), efficiently inhibits cutaneous metastatic melanoma (CMM).
DC74249 TAS0612 TAS0612 (TAS-0612) is an orally bioavailable multikinase inhibitor of AKT, p70S6K, and p90RSK, inhibits Y-box-binding protein (YBX1) phosphorylation.
DC74250 TCMDC-136364 TCMDC-136364 (AKT Kinase Inhibitor) is an Akt kinase inhibitor, selectively inhibits Akt in proliferating cells expressing Trop-2, also potently inhibits P. falciparum multidrug resistant strain Dd2.
DC74251 BI-9774 Featured BI-9774 (BI 9774) is a potent pan-AMPK activator with EC50 of 64 nM in an ADP-Glo kinase assay with human AMPK (α1β1γ1) and EC50 of 8 nM in a cellular GLUT4 translocation assay.
DC74252 KI-301670 KI-301670 is a novel potent, specific NUAK1 inhibitor, disturbs NUAK1 signaling by targeting its ATP binding site, effectively inhibits the PI3K/AKT pathway in pancreatic cancer cells.
DC74253 MSG011 MSG011 is a potent, pan AMPK isoform activator with EC50 of 140.4 nM, 248.9 nM, 553.4 nM, and 472.9 nM for α1β1γ1, α1β2γ1, α2β1γ1, and α2β2γ1, respectively.
DC74254 PXL770 PXL770 is a novel orally bioavailable, small-molecule direct AMPK activator with EC50 of 16.2, 42.1 and 64 nM for α1β1γ1, α1β1γ2 and α1β1γ3, directly increases AMPK activity by both allosteric activation and protection from dephosphorylation.
DC74255 PXL770 monohydrate potassium salt PXL770 is a novel orally bioavailable, small-molecule direct AMPK activator with EC50 of 16.2, 42.1 and 64 nM for α1β1γ1, α1β1γ2 and α1β1γ3, directly increases AMPK activity by both allosteric activation and protection from dephosphorylation.
DC74256 RX-375 RX-375 (RX375) is an indirect small-molecule activator of AMPK by directly binds to Prohibitins (PHB1 and PHB2), induces dissociation of AMPK-PHBs complex.
DC74257 ZLN-024 hydrochloride ZLN-024 hydrochloride is a potent, allosteric AMPK activator that has no effect on mitochondrial function or the ADP/ATP ratio, directly activate recombinant AMPK α1β1γ1 and its homologue α2β1γ1 with EC50 of 0.42 uM and 0.95 uM, respectively.
DC74258 NV-5297 NV-5297 (NV5297) is a novel small molecule mTORC1 pathway activator, modulates the Sestrin2-Gator2 interaction and activates the mTORC1 pathway in vitro and in vivo.
DC74259 CU05-1189 CU05-1189 is a non-peptide, allosteric inhibitor of the pleckstrin homology (PH) domain of PDK1, specifically inhibits Akt signaling pathway.
DC74260 cyclo-CRVLIR Featured cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.
DC74261 HM5023507 HM5023507 is a potemt, selective, orally active dual PI3Kδ/γ inhibitor with IC50 of 4 nM and 5 nM for p110γ and p110δ, respectively.
DC74262 I-229 I-229 is a potent and selective inhibitor of Vps34.
DC74263 LL-00071210 LL-00071210 is a potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 values of 24.6 nM and 9.4 nM in biochemical and cellular assays, respectively.
DC74264 LL-00084282 LL-00084282 is a potent, selective and efficacious dual PI3Kδγ inhibitor with IC50 of 16.26 and 17.45 nM for PI3Kδ and PI3Kγ, respectively.
DC74265 LP-182 LP-182 (LP182) is a potent, selective and orally bioavailable multi-functional kinase inhibitor, specifically targets PI3K and MAPK signaling pathways.
DC74266 PF-06862309 PF-06862309 (PF-06843195 phosphate ester prodrug) is the in vivo-active, phosphate ester prodrug of PF-06843195, a potent selective PI3Kα inhibitor with Kd of <18 pM.
DC74267 PITCOIN2 PITCOIN2 (LU-06-006) is a potent selective PI3KC2α inhibitor with IC50 of 126 nM, has selectivity against PI3KC2γ but shows micromolar activity on PI3KC2β.
DC74268 PITCOIN3 PITCOIN3 is a potent, highly selective, cell-permeable inhibitor of PI3KC2α catalytic activity with IC50 of 126 nM.
DC74269 TGX286 TGX286 is a potent, selective p110β inhibitor with IC50 of 7, 17 and 13 nM for p110β WT, p110β D862Q, and p110β E858H, respectively, >100-fold selectivity over p110α.
DC74270 GSK-3923868 GSK-3923868 (PI4KB inhibitor 30) is a potent, selective, slow-dissociating PI4KB (PI4kIII-beta) inhibitor with pKi of 9.8, >1000-fold selectivity over PI4KA, inhibits HRV viral replication in COPD BECs.
DC74271 HZX-02-059 HZX-02-059 is a PIKfyve and tubulin dual-target inhibitor with high affinity for PIKfyve (Kd=10.4 nM), HZX-02-059 is a potent methuosis inducer, shows both in vitro and in vivo anti-tumor activity against TNBC.
DC74272 BAY-728 BAY-728 (NAY728) is a less potent enantiomer and negative control compound of BAY-805.
DC74273 BK50118-C BK50118-C is a potent small molecule inhibitor of ubiquitin-specific protease-13 (USP13) with IC50 of 0.42 nM.
DC74274 BML-260 BML-260 (BML260) is a potent inhibitor of dual-specific phosphatase JSP-1 (JNK Stimulatory Phosphatase-1, DUSP22) and stimulator of uncoupling protein 1 (UCP-1) expression in adipocytes.

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