Cercosporamide A selective and potent MNK, Pkc1, and JAK3 inhibitor

Cercosporamide (CAS 131436-22-1)

Cercosporamide | CAS 131436-22-1 is rated 5.0 out of 5 by 1.
  • y_2019, m_7, d_20, h_20
  • bvseo_bulk, prod_bvrr, vn_bulk_2.0.12
  • cp_1, bvpage1
  • co_hasreviews, tv_0, tr_1
  • loc_en_US, sid_202095, prod, sort_[SortEntry(order=SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getAggregateRating, 41ms
  • REVIEWS, PRODUCT
Synonym: (R)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9aβ-methyl-9-oxodibenzofuran-4-carboxamide
Application: A selective and potent MNK, Pkc1, and JAK3 inhibitor
CAS Number: 131436-22-1
Purity: >95%
Molecular Weight: 331.3
Molecular Formula: C16H13NO7
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

Cercosporamide, an usnic amide, was originally identified in Cercosporidium henningsii as a host-selective phytotoxin and broad-spectrum antifungal agent and is a potent inhibitor of MAP-kinase interacting kinase-2 (Mnk2; IC50 = 11 nM), JAK3 (IC50 = 31), and Mnk1 (IC50 = 116 nM). This compound inhibits fungal wall synthesis via targeting of β-1,3-glucan synthase and is reported to exhibit a different mode of action as compared to azole-based fungal inhibitors. Cercosporamide is additionally noted to act as a selective and potent fungal Pkc1 inhibitor and may provide insight as to how Saccharomyces cerevasiae cell-wall mutants become sensitive to this compound. Additional studies in S. cerevisiae have reported that cercosporamide is useful in researching the KNR4 gene in the synthesis of the yeast cell wall. Minimum inhibitory concentration (MIC) as reported using LV-2841, an unidentified fungal culture producing cercosporamide, is reported to be 8-16 μg/mL.


References

1. Hong, Z., et al. 1994. Mol. Cell. Biol. 14: 1017-1025. PMID: 8289782
2. Sussman, A., et al. 2004. Eukaryotic Cell. 3: 932-943. PMID: 15302826
3. Hoffman, A.M., et al. 2008. Phytochemistry. 69: 1049-1056. PMID: 18070629
4. Furukawa, A., et al. 2009. Bioorg. Med. Chem. Lett. 19: 724-726. PMID: 19109017
6. Singh, M.P., et al. 2010. J. Ind. Microbiol. Biotechnol. 37: 335-340. PMID: 20033470

Appearance :
Lyophilized
Physical State :
Solid
Derived From :
Cercosporidium sp. MST-FP1899
Solubility :
Soluble in ethanol, methanol, DMSO ( 5 mg/ml, solution in DMSO is unstable and thus should be freshly prepared.), DMF, chloroform (1 mg/ml), and ethyl acetate (1 mg/ml).
Storage :
Store at -20° C
Melting Point :
257.66° C (Predicted)
Boiling Point :
582.53° C at 760 mmHg
Density :
1.71 g/cm3
Refractive Index :
n20D 1.74 (Predicted)
IC50 :
Protein kinase C-like 1: IC50 = 44 nM (Candida albicans); Protein kinase C beta: IC50 = 350 nM (human); Protein kinase C alpha: IC50 = 1020 nM (human); Protein kinase C gamma: IC50 = 5800 nM (human); Pkc1 kinase: IC50 = < 50 nM
pK Values :
pKa: 11.89
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
131379
MDL Number :
MFCD14635433
SMILES :
CC(=O)C1=C(C=C2[C@@](C1=O)(C3=C(C=C(C(=C3O2)C(=O)N)O)O)C)O

Download SDS (MSDS)

Certificate of Analysis

Adobe Acrobat Reader is required to reliably view,
print and comment on PDF documents

Cercosporamide  Product Citations

See how others have used Cercosporamide. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 26468616  Darieva, Z. et al. 2015. Elife. 4: e09886.

PMID: # 26824022  Müller, D. et al. 2013. Translation (Austin). 1: e25819.

Citations 1 to 2 of 2 total
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getContent, 67ms
  • QUESTIONS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;
Rated 5 out of 5 by from Altman Altman, JK. et al. (PubMed 23509154) investigated whether Cercosporamide, a selective and potent MNK, Pkc1, and JAK3 inhibitor, exhibited any anti-leukemic properties. They found that Cercosporamide suppresses phosphorylation of eIF4E and exhibits antileukemic effects. -SCBT Publication Review
Date published: 2015-03-13
  • y_2019, m_7, d_20, h_20
  • bvseo_bulk, prod_bvrr, vn_bulk_2.0.12
  • cp_1, bvpage1
  • co_hasreviews, tv_0, tr_1
  • loc_en_US, sid_202095, prod, sort_[SortEntry(order=SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getReviews, 39ms
  • REVIEWS, PRODUCT

Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2019 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.