IKK 16

IKK 16 is an orally active IKK inhibitor. IKK 16 shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 protects against LPS -induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway[1][2][3][4][5][6][7].

873225-46-8

12352005

H315, H319, H320

IKK; Interleukin Related; LRRK2; NF-κB; P-glycoprotein; PKD; TNF Receptor

Reference compound

Apoptosis; Autophagy; Immunology/Inflammation; Membrane Transporter/Ion Channel; NF-κB

COVID-19-immunoregulation

Inflammation/Immunology; Cardiovascular Disease

https://www.medchemexpress.com/IKK-16.html

99.88

DMSO : ≥ 27 mg/mL

O=C(C1=CC=C(NC2=NC=CC(C3=CC4=CC=CC=C4S3)=N2)C=C1)N5CCC(N6CCCC6)CC5

C28H29N5OS

483.63

H315, H319, H320

[1]Amaro-Leal Â, et al. Therapeutic effects of IkB kinase inhibitor during systemic inflammation. Int Immunopharmacol. 2020 Jul;84:106509. |[2]Johnson FL, et al. Inhibition of IκB Kinase at 24 Hours After Acute Kidney Injury Improves Recovery of Renal Function and Attenuates Fibrosis. J Am Heart Assoc. 2017 Jul 3;6 (7) :e005092. |[3]Waelchli R, et al. Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorg Med Chem Lett. 2006 Jan 1;16 (1) :108-12. |[4]Hermanson SB, Carlson CB, Riddle SM, Zhao J, Vogel KW, Nichols RJ, Bi K. Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PLoS One. 2012;7 (8) :e43580. |[5]SURA AL ZOUBI, et al. Inhibition of NF-κB Pathway with IKK-16 or Linagliptin Attenuates the Cardiac Dysfunction Associated with Polymicrobial Sepsis in Mice with Preexisting Type 2 Diabetes Mellitus (T2DM) . Diabetes 1 July 2018; 67 (Supplement_1) : 483–P. |[6]Tandon M, et al. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells. PLoS One. 2013 Sep 23;8 (9) :e75601.|[7]Ansbro MR, et al. Screening compounds with a novel high-throughput ABCB1-mediated efflux assay identifies drugs with known therapeutic targets at risk for multidrug resistance interference. PLoS One. 2013 Apr 10;8 (4) :e60334.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

Reference compound1

No Development Reported