Molecular Formula | C13H11NO4 |
Molar Mass | 245.23 |
Solubility | DMSO: ≥ 34 mg/mL |
Appearance | White to light yellow powder |
Color | white to beige |
Storage Condition | room temp |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
In vitro study | In COLO 320DM (human colon cancer) cells, KNK437 dose-dependently inhibited the acquisition of Thermotolerance and the activity of individual HSPs, including Hsp105, HSP70 and hsp40. KNK437 and quercetin dose-dependently inhibited Thermotolerance in PC-3 cells. KNK437 reduced heat-induced accumulation of HSP70 mRNA and protein in PC-3 and LNCaP cells. |
In vivo study | KNK437(200 mg/kg, I. P.) showed no anti-tumor effect and did not increase the temperature sensitivity of non-resistant tumors. The same dose of KNK437 synergistically increased the anti-tumor efficacy of the graded heat treatment. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.078 ml | 20.389 ml | 40.778 ml |
5 mM | 0.816 ml | 4.078 ml | 8.156 ml |
10 mM | 0.408 ml | 2.039 ml | 4.078 ml |
5 mM | 0.082 ml | 0.408 ml | 0.816 ml |
Introduction | KNK437 (218924-25-5) Inhibits Constitutive and inducible HSP70 expression in non-stressed and heat-stressed cancer cells. Blocks geldanamycin-induced HSP70 induction and inhibition of TGF signaling. Inhibition of leukocyte integrin α-7-mediated T cell adhesion to Mucosal addressin cell adhesion molecule 1 (MAdCAM-1) suggests that HSP70 is critical for 7 integrin signaling. Inhibits morphine analgesia tolerance in a rodent model (100 mg/Kg). |
biological activity | KNK437 is a pan-HSP inhibitor that inhibits inducible HSPs, including HSP105,HSP72, and synthesis of hsp40. |
Target | TargetValue HSP105 () HSP72 () HSP40 () |
Target | Value |
in vitro study | in COLO 320DM (human colon cancer) cells, KNK437 dose-dependently inhibited the acquisition of Thermotolerance and the activity of individual HSPs, including Hsp105, HSP70 and hsp40. KNK437 and quercetin dose-dependently inhibited Thermotolerance in PC-3 cells. KNK437 reduced heat-induced accumulation of HSP70 mRNA and protein in PC-3 and LNCaP cells. |
in vivo studies | KNK437(200 mg/kg, I. P.), and does not increase the temperature sensitivity of non resistant tumors. The same dose of KNK437 synergistically increased the anti-tumor efficacy of the graded heat treatment. |