MALT1 paracaspase inhibitor 3 is a potent, specific, covalent inhibitor of MALT1 paracaspase with Ki of 10 nM, exhibits 10-and 100-fold improved potency in vitro and in vivo compared with Z-VRPR-fmk.

MI 2(MALT1 inhibitor) is a small molecule and irreversible inhibitor of MALT1 with IC50 of 5.84 uM(suppression of proliferation in ABCDLBCL).

MI-2 is an inhibitor of MALT1 with IC50 value of 5.84 μM.

NIK SMI1 is a potent, selective small molecule inhibitor of NF-κB inducing kinase (NIK) with Ki of 230±170 pM; only inhibits 3 out of 222 off-target kinases (KHS1, LRRK2, and PKD1) with >75% inhibition at 1 uM; potently inhibits anti-LTβR-induced nuclear p52 levels in anti-LTβR-stimulated HeLa cells, with no effect on canonical signaling; inhibits BAFF and CD40 signaling, suppresses immune responses in vivo; suppresses disease biomarkers and improves survival and renal function in NZB/W F1 mice.

PS-1145 has been shown to be an IKK (IKB kinase) inhibitor.

SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM.

Takinib is a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease.

TPCA-1 is potent, selective inhibitor of IKK-2 (IC50 = 17.9 nM) that displays>22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes.

Triptolide is the major bioactive constituent of T. wilfordii Hook F., also known as thunder god vine, a traditional Chinese medicinal herb with known antiproliferative, immunosuppressive, anti-inflammatory, antifertility, and anti-polycystic kidney disea

WS3 is a novel small molecule that promotes β cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).

WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

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.

Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.

B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor with a Ki of 4.2 nM. B022 protects liver from toxin-induced inflammation, oxidative stress, and injury.

Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity.

Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.

DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.

BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy.

(Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy.

HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.

BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases.

Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.