IKK 16 (hydrochloride)
CAS No. : 1186195-62-9
| Size | Price | Stock |
|---|---|---|
| 5mg | $100 | In-stock |
| 10mg | $174 | In-stock |
| 25mg | $320 | In-stock |
| 50mg | $520 | In-stock |
| 100mg | $740 | In-stock |
| 200mg | $1050 | In-stock |
| 500 mg | Get quote | |
| 1 g | Get quote | |
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| Cat. No. : | HY-13687A |
| M.Wt: | 520.09 |
| Formula: | C28H30ClN5OS |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride 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].
IC50 & Target:IC50: 40 nM (IKK2), 70 nM (IKK complex), 200 nM (IKK1)[1]
IC50: 50 nM (LRRK2)[2]
In Vitro:IKK 16 hydrochloride inhibits IκB degradation and inhibits TNFα-stimulated E-Sel, ICAM, VCAM, β2M, and HLA-DR expression in HUVEC cells, with IC50s of 1, 0.5, 0.3, 0.3, 2, 2 μM, respectively[3].
IKK 16 hydrochloride (20 μM) inhibits phosphorylation of Ser910, Ser935, Ser955 and Ser973 in Flp-In T-REx™ HEK293 GFP-LRRK2 G2019S cells[4].
IKK 16 hydrochloride (20 μM) rescues phosphorylation of Ser910, Ser935, Ser955 and Ser973 in Flp-In T-REx™ HEK293 LRRK2 A2016T/G2019S mutant[4].
IKK 16 hydrochloride (1 μM) inhibits PKD1 activity by 67%,is ATP-competitive inhibitors[6].
IKK 16 hydrochloride (1-100 μM) inhibits PKCα and PKCδ[6].
In Vivo:IKK 16 hydrochloride (1 mg/kg, i.v., once) protects against LPS-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure in male Wistar rats model[1].
IKK 16 hydrochloride (1 mg/kg, i.v., once) improves recovery of renal glomerular and tubular function, prevents fibrosis at 28 days after the AKI insult in male Wistar rats model[2].
IKK 16 hydrochloride (30 mg/kg, s.c., once) suppresses systemic TNFα levels in LPS-induced rats model[3].
IKK 16 hydrochloride (10 mg/kg, s.c., once) inhibits neutrophil extravasation in thioglycollate-induced peritonitis mice model[3].
IKK 16 hydrochloride reduces CLP-induced cardiac dysfunction, NF-κB pathway activation and iNOS expression in high fat (HFD)-caecal ligation and puncture (CLP) mice model[5].
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