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Malformin C

Antibiotic
 
ALX-380-318-M001 1 mg Inquire for pricing
 
ALX-380-318-MC25 0.25 mg Inquire for pricing
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Inhibitor of bleomycin-induced G2 arrest. Has antibacterial, antimalarial and antitrypanosomal activity. Induces root curvature and malformation in plants and enhances fibrinolytic activity in plants.

Product Specification

Alternative Name:(-)-cyclo[D-Cys(1)-D-Cys(1)-L-Val-D-Leu-L-Leu-]
 
Formula:C23H39N5O5S2
 
MW:529.7
 
Source:Synthetic. Originally isolated from Aspergillus niger FKI-2342.
 
CAS:59926-78-2
 
Purity:≥97% (HPLC)
 
Appearance:White solid.
 
Solubility:Soluble in 100% ethanol, chloroform, DMSO or methanol; insoluble in water.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Scientific Background:Spontaneous and chemical damage to DNA induces signal-transduction pathways called checkpoints. Once activated, DNA-damage checkpoint signaling delays cell cycle progression and initiates the repair of the damaged DNA. DNA damage in normal human cells can be repaired in both the G1 and G2 phase. In contrast, most cancer cells can restore DNA damage only in the G2 phase due to mutations in genes responsible for encoding pivotal proteins of the G1 checkpoint. Therefore, G2 checkpoint inhibitors in cancer cells are expected to be selective potentiators of DNA-damaging agents and thus might emerge as highly useful compounds for cancer research.

Malformin C is a bicyclic pentapeptide containing L-leucine, D-isoleucine, L-valine, and two D-cysteins coupled with a disulfide-bond bridge. Malformins A1 and and C, originally isolated from the culture broth of Aspergillus niger FKI-2342, were found to abrogate the bleomycin (Prod. No. BML-AP302)-induced G2 arrest in Jurkat cells with IC50 values of 480nM and 0.9nM, respectively. Therefore, malformins may be promising candidates as anti-cancer agents.
 
Technical Info/Product Notes:Synthesized by the Organic Chemistry Group, The Kitasato Institute.
 
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Product Literature References

Solid-phase synthesis and biological activity of malformin C and its derivatives: Y. Kojima, et al.; J. Antibiot. (Tokyo) 62, 681 (2009), Abstract;
Total synthesis of malformin C, an inhibitor of bleomycin-induced G2 arrest: Y. Kojima, et al. ; J. Antibiot. (Tokyo) 61, 297 (2008), Abstract;
Fungal malformins inhibit bleomycin-induced G2 checkpoint in Jurkat cells: K. Hagimori, et al. ; Biol. Pharm. Bull. 30, 1379 (2007), Abstract;
Enhancement of fibrinolytic activity of U937 cells by malformin A1: Y. Koizumi & K. Hasumi; J. Antibiot. (Tokyo) 55, 78 (2002), Abstract;
Antibiotic properties of malformin: S. Suda & R.W. Curtis ; Appl. Microbiol. 14, 475 (1966), Abstract; Full Text
Curvatures and Malformations in Bean Plants Caused by Culture Filtrate of Aspergillus niger: R.W. Curtis ; Plant Physiol. 33, 17 (1958), Abstract; Full Text
Root curvatures induced by culture filtrates of Aspergillus niger: R.W. Curtis ; Science 128, 661 (1958), Abstract;

General Literature References

Cell cycle control and cancer.: L. H. Hartwell & M. B. Kastan; Science 266, 1821 (1994), Abstract;

Related Products

Bleomycin sulfate 

Antitumor antibiotic
9041-93-4, ≥98% (HPLC) | Print as PDF
 
BML-AP302-0010 10 mg 281.00 USD
 
BML-AP302-0050 50 mg 989.00 USD
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