Custom Enzymes and Inhibitors
Selleck Chemical LLC Olaparib (AZD2281) 100mg 763113-22-0 Ku-0059436
Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC TWS119 10mg 601514-19-6
TWS119 is a GSK-3? inhibitor with IC50 of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3? inhibition triggers autophagy. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Resveratrol 500mg 501-36-0
Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 ?M), lipooxygenases(LOX, IC50=2.7 ?M), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Doramapimod (BIRB 796) 50mg 285983-48-4
Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38?/?/?/? in cell-free assays, and binds p38? with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC BI 2536 50mg 755038-02-9
BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC TW-37 10mg 877877-35-5
TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 ?M, 1.11 ?M and 0.26 ?M in cell-free assays, respectively. *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 Luminespib (NVP-AUY922) 5mg 747412-49-3 AUY-922
Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90?/? with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1R? protein and results in growth inhibition, autophagy and apoptosis. Phase 2. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Luminespib (NVP-AUY922) 25mg 747412-49-3 AUY-922
Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90?/? with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1R? protein and results in growth inhibition, autophagy and apoptosis. Phase 2. *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 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 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 SP600125 10mg 129-56-6 Nsc75890
SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKC?, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad?spectrum inhibitor of serine/threonine kinases including Aurora kinase A,FLT3 and TRKA with of IC50 of 60?nM, 90?nM and 70?nM. SP600125 inhibits autophagy and activates apoptosis. *For Research & Development use only. Product is not intended for drug, household, or human consumption.
Selleck Chemical LLC Temsirolimus (CCI-779) 10mg 162635-04-3 NSC 683864
Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 ?M in a cell-free assay. Temsirolimus induces autophagy and apoptosis. *For Research & Development use only. Product is not intended for drug, household, or human consumption.