| Cat. No. |
Product Name |
CAS No. |
Information |
| H5612 |
WS-6
|
1421227-53-3 |
A small molecule that can induce proliferation of β cells with EC50 of 0.28 uM; promotes β cell growth in vivo, increasing β cell mass and normalizing blood glucose in the RIP-DTA mouse model of β cell ablation; acts by inhibiting IKKε and blocking the ability of EBP1 to suppress E2F-medtiated transcription; also stimulates α cell proliferation in human pancreatic islets. |
| H5611 |
WS-3
|
1421227-52-2 |
A small molecule that can induce proliferation of β cells with EC50 of 74 nM; modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway; can reversibly proliferates primary RPE cells isolated from fetal and adult human donors. |
| H5610 |
TPCA-1
|
507475-17-4 |
A potent, selective and orally bioavailable IKK-2 inhibitor with IC50 of 63 nM, TNF cell IC50 of 0.4 uM; displays >100-fold selectivity over IKK-1. |
| H5609 |
TBK1-IN-1
|
1292310-49-6 |
TBK1-IN-1 is a potent, ATP-competitive TBK1 inhibitor, dose-dependently inhibits pIRF3(S386) in Panc 05.04 cells with IC50 of 1.8 nM; inhibits IRF3 nuclear translocation with IC50 of 95 nM, but does not significantly inhibits cell proliferation in some NSCLC, pancreatic, and colorectal cell lines. |
| H5608 |
TBK1-IKKε inhibitor II
|
1381930-17-1 |
TBK1-IKKε inhibitor II is a potent, selective dual inhibitor of TBK1/IKKε with IC50 of 13 nM/59 nM, respectively; displays 100- to 1000-fold less activity against other tested protein kinases including PDK1, PI3K family members and mTOR; inhibits LPS-induced expression of IFNβ (IC50=62 nM), and the IFNβ target genes IP10 (IC50=78 nM) and Mx1 (IC50=20 nM); effectively blocks TLR3-dependent IRF3 nuclear translocation in cells with IC50
|
| H5607 |
SU-909
|
2126749-48-0 |
SU-909 (SU909, IKKα-IN-48) is a potent, selective IKKα inhibitor with Ki of 0.08±0.07 uM, 10-20-fold selectivity over IKKβ (IC50=1.0±0.28 uM); inhibits FCS-stimulated phosphorylation of p100 in U2OS cells with IC50 of 8.8 uM, inhibits the noncanonical NF-kB pathway without affecting IKKβ-dependent IKappa-Bα loss in the canonical pathway. |
| H5606 |
PS-1145
|
431898-65-6 |
A specific IκB kinase (IKK) inhibitor with IC50 of 88 nM; shows no activity for JNK2, c-Src, p38α, IRAK, Lck, etc.; blocks TNFα-induced NF-κB activation in MM cells through inhibition of IκBα phosphorylation and degradation of IκBα, respectively; blocks the protective effect of IL-6 against Dex-induced apotosis, inhibits both IL-6 secretion from BMSCs triggered by MM cell adhesion and proliferation of MM cells adherent to BMSCs. |
| H5605 |
PIAA
|
851814-28-3 |
PIAA is a TBK1/IKKε inhibitor with IC50 of 0.40/1.07 uM, selectively accelerates proliferation of β-cells; downregulates polyinosine:polycytidylic acid (poly I:C)-stimulated phosphorylation of interferon responsive factor-3 (IRF3), a substrate of TBK1/IKKε; augments β-cell-specific proliferation by increasing cAMP levels and mTOR activity via PDE3, improves glucose control and β-cell mass in the STZ-induced diabetic mouse model. |
| H5604 |
PHA-408
|
503555-55-3 |
A novel potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1; inhibits LPS-induces TNF-α producton in PBMCs and HWB with IC50 of 20-30 nM, prevents IL-1β-induced IκBα phosphorylation in RASFs while sparing the JNK and p38 MAPK pathways and has no effect on IKK-2 phosphorylation; demonstrates target-specific anti-inflammatory activities in in vivo model of airway inflammation. |
| H5603 |
iNUB
|
352336-00-6 |
A small molecule inhibitor of NEMO (IKKγ)-ubiquitin binding with EC50 of 9.3 uM, directly binds to NEMO with Kd of 2.14 uM; binds to NEMO UBAN (ubiquitin binding domain (UBAN)) and competes for interaction with methionine-1-linked linear ubiquitin chains; inhibits UBAN-dependent NF-κB activation upon TNFα and TCR/CD28 stimulation, shows selective toxicity to IKK/NF-κB dependent ABC-DLBCL |
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