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Purity: ≥98%
KNK437 (KNK-437; KNK 437; Heat Shock Protein Inhibitor I), a benzylidene lactam analog, is a novel and potent pan-HSP (heat shock proteins) inhibitor with potential antineoplastic activity. KNK-437 inhibited the acquisition of thermotolerance and the induction of various HSPs such as HSP105, HSP70, and HSP40 in a dose-dependent manner in COLO 320DM (human colon carcinoma) cells.
| ln Vitro |
In COLO 320DM (human colon cancer) cells, KNK437 suppresses the activation of multiple HSPs, such as HSP105, HSP70, and HSP40. Following the initial heat treatment, COLO 320DM cells' ability to tolerate heat is inhibited by KNK437 (100 μM). In COLO 320DM cells (0-200 μM) and HeLa S3 cells (100, 200 μM), KNK437 exhibits dose-dependent inhibition of thermotolerance [1]. When applied pre- and post-heat, KNK437 (100 μM) inhibits the methylation of H3-Lys4 in HSC4 and KB cells, but has no effect on H3 Lys9 methylation. HSP70 expression is also inhibited by KNK437 [3].
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| ln Vivo |
It is a weak agent, KNK437. Tumor-free CD-1 (ICR) mice regain body weight loss when given KNK437 (62.5-400 mg/kg). In tumors that were heat intolerant, KNK437 (200 mg/kg) did not enhance heat sensitivity or have any anticancer effects. The anticancer effect of fractionated heat treatment at 200 mg/kg at 44°C is synergistically enhanced by KNK437. The administration of KNK437 (200 mg/kg, i.p.) six hours prior to the beginning heating process reduces thermotolerance [2].
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| Animal Protocol |
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| References |
[1]. Yokota S, et al. Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and heat shock protein induction in human colon carcinoma cells. Cancer Res. 2000 Jun 1;60(11):2942-8.
[2]. Koishi M, et al. The effects of KNK437, a novel inhibitor of heat shock protein synthesis, on the acquisition of thermotolerance in a murine transplantable tumor in vivo. Clin Cancer Res. 2001 Jan;7(1):215-9. [3]. Matsuda K, et al. Effects of KNK437 on heat-induced methylation of histone H3 in human oral squamous cell carcinoma cells. Int J Hyperthermia. 2006 Dec;22(8):729-35 |
| Molecular Formula |
C13H11NO4
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| Molecular Weight |
245.23
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| CAS # |
218924-25-5
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| Related CAS # |
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| SMILES |
O=CN1C(/C(CC1)=C\C2=CC=C(OCO3)C3=C2)=O
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| InChi Key |
NJBBLOIWMSYVCQ-VZTVMPNDSA-N
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| InChi Code |
InChI=1S/C33H41N5O6S2/c1-33(2,3)37-31(42)26-19-46-20-38(26)32(43)29(40)24(15-21-9-6-5-7-10-21)36-30(41)25(18-45-4)35-28(39)17-44-27-12-8-11-22-16-34-14-13-23(22)27/h5-14,16,24-26,29,40H,15,17-20H2,1-4H3,(H,35,39)(H,36,41)(H,37,42)/t24-,25-,26-,29-/m0/s1
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| Chemical Name |
(Z)-3-(benzo[d][1,3]dioxol-5-ylmethylene)-2-oxopyrrolidine-1-carbaldehyde
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| Synonyms |
KNK437; KNK 437; KNK-437;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0778 mL | 20.3890 mL | 40.7780 mL | |
| 5 mM | 0.8156 mL | 4.0778 mL | 8.1556 mL | |
| 10 mM | 0.4078 mL | 2.0389 mL | 4.0778 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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