|Targets||IKK | PDK-1|
|Description||BX795 is a potent and selective inhibitor of PDK1, IKKε and TBK1, which regulates the production of Type 1 interferons during bacterial and viral infection. BX795 blocks the phosphorylation, nuclear translocation, and transcriptional activity of interferon regulatory factor 3 and the production of interferon-β in macrophages stimulated with poly(I:C) or lipopolysaccharide (LPS). BX795 also inhibits ERK8, MAPK-interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-regulating kinases 1-4, TNF receptor associated factor-associated NF-κB activator-binding kinase 1.|
|B0084-194478||25 mg||$189||In stock|
|Brife Description||PDK1/IKKε/TBK1 inhibitor|
|Synonyms||BX-795; BX 795; BX795. N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide|
BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1. It exhibits no effect against a panel of 15 other kinases and attenuate...
OSU 03012, a Phenanthren derivative, has been found to be a PDPK1 inhibitor that could probably be an effctive antitumor agent. It is still under Phase I trail ...
TEPP-46, an effective sensitizer of recombinant pyruvate kinase M2, has been found to decrease the formation of tumor in a mouse xenograft model. IC50: 92 nM (A...
ML 120B dihydrochloride
ML 120B dihydrochloride is an ATP-competitive IKK2-selective inhibitor with IC50 value of 60 nM at 50 μM ATP. It can inhibit paw swelling, bone and cartilage de...
TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM and 0.40 μM for IKK-1 and IKK-2 respectively. It blocks NF-κB pathway and STAT3 activity.
IKK16 is a selective IκB kinase (IKK) inhibitor for IKK-2( IC50=40 nM), IKK complex( IC50=70 nM) and IKK-1(IC50=2000 nM).
BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.
PHA 408 is a selective and ATP-competitive IKB kinase-2 (IKK-2) inhibitor (IC50 = 40 nM), which binds IKK-2 tightly with a relatively slow off rate.