Custom Enzymes and Inhibitors
Echelon Biosciences Research Labs LY294002 (HCI SALT) 5 mg
LY294002 is a selective, cell permeable, potent and specific inhibitor of phosphatidylinositol 3-kinase (IC50 = 1.4 M; purified PI 3-kinase). It does not significantly inhibit PKC, PKA, MAP kinase, S6 kinase, EGFrK, c-src kinase, PI 4-kinase, DAG kinase or rabbit kidney ATPase at concentrations of 50 M. Induces apoptosis. In intact neutrophils stimulated with fMet-Leu-Phe, LY294002 completely abolished PI 3-kinase activity at 50 M without cell toxicity.nn
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Specifications
nProvided as HCl saltnNot SterilenFeatured in Publications
nDocuments
nTechnical Data Sheet This item is non returnable
Selleck Chemical LLC SNS-314 5mg 1057249-41-8
SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Nutlin-3 25mg 890090-75-2
Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Diclofenac Sodium 50mg 15307-79-6 GP 45840
Diclofenac Sodium (GP 45840) is a non-selective COX inhibitor with IC50 of 0.5 ?g/ml and 0.5 ?g/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Dutasteride 10mg 164656-23-9 GI198745, GG-745
Dutasteride (GI198745, GG-745) is a dual 5-? reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT). *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Posaconazole 5mg 171228-49-2 SCH56592
Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14? demethylase inhibitor with IC50 of 0.25 ?M. Posaconazole has a median terminal elimination half-life of 15-35 hours. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Foretinib (GSK1363089) 50mg 849217-64-7 EXEL-2880,XL-880
Foretinib (GSK1363089, EXEL-2880, XL-880) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFR?/? and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Roflumilast 5mg 162401-32-3 APTA 2217, B9302-107, BY 217, BYK 20869
Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC GDC-0879 5mg 905281-76-7 AR-00341677
GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Rucaparib (AG-014699) phosphate 10mg 459868-92-9 PF-01367338
Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Roscovitine (Seliciclib) 50mg 186692-46-6 CYC202
Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 ?M, 0.7 ?M and 0.16 ?M in cell-free assays. It shows little effect on CDK4/6. Phase 2. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC PLX-4720 25mg 918505-84-7
PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC CUDC-101 10mg 1012054-59-9
CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC ABT-737 50mg 852808-04-9
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Tozasertib (VX-680, MK-0457) 25mg 639089-54-6
Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2. *For Research & Development use only. Product is not intended for drug, household, or human consumption.