BML-275 A potent inhibitor of AMPK and fatty acid biosynthesis

BML-275 (CAS 866405-64-3)

BML-275 | CAS 866405-64-3 is rated 5.0 out of 5 by 1.
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Synonym: Dorsomorphin
Application: A potent inhibitor of AMPK and fatty acid biosynthesis
CAS Number: 866405-64-3
Purity: ≥98%
Molecular Weight: 399.49
Molecular Formula: C24H25N5O
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and Fatty Acid Synthase inhibitor. Phosphorylation of AMPK occurs in vivo when energy sources are low and in-turn suppresses expression of SREBP-1. SREBP-1 is a key lipogenic transcription factor, and its suppression allows glucose production by hepatocytes. In mouse studies it has been reported that BML-275 rapidly reduces the level of the phosphorylated AMPK α subunit in the hypothalamus, in an ATP-competitive manner, therefore altering energy perception and affecting the physiological energy sensor of the body. Over-activation of AMPK has also been found to be deleterious in ischemic stroke conditions and inhibition of AMPK by BML-275 may provide a small level of neuroprotection. Additional research on zebrafish has shown that BML-275 also inhibits bone morphogenetic protein signals required for iron metabolism and embryogenesis. BML-275 is an inhibitor of ACTR-I, BMPR-IA and BMPR-IB.


References

1. Zhou, G., et al. 2001. J. Clin. Invest. 108: 1167-1174. PMID: 11602624
2. Kim, E.K., et al. 2004. J. Biol. Chem. 279: 19970-19976. PMID: 15028725
3. McCullough, L.D., et al., 2005. J. Biol. Chem. 280: 20493-20502. PMID: 15772080
4. Ramamurthy, S. and Ronnett, G.V. 2006. J. Physiol. 574: 85-93. PMID: 16690704
5. Yu, P.B., et al. 2008. Nat. Chem. Biol. 4: 33-41. PMID: 18026094

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (4 mg/ml warm), 100 mM HCl, and MeOH.
Storage :
Store at -20° C
Melting Point :
244.93° C
Boiling Point :
569.21° C
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.67
IC50 :
KDR/VEGFR2: IC50 = 25.1 nM; ALK2/BMPR-I: IC50 = 148 nM; AMPK kinase: IC50 = 234.6 nM; VEGF signaling-dependent intersomitic vessel formation: EC5050 = 2 µM
Ki Data :
AMP kinase: Ki= 109 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
11524144
MDL Number :
MFCD08705402
SMILES :
C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3

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Certificate of Analysis

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BML-275  Product Citations

See how others have used BML-275. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 21 total

PMID: # 28675237  Chen, J. et al. 2017. Food Funct. 8: 2425-2436.

PMID: # 2644975228729840  Marczenke, M. et al. 2017. Front Physiol. 8: 469.

PMID: # 26803770  Malan, D. et al. 2016. Basic Res. Cardiol. 111: 14.

PMID: # 26486079  2015. Oncotarget. 6: 39692-701.

PMID: # 25750208  Sugawa, F. et al. 2015. The EMBO journal. 34: 1009-24.

PMID: # 25639979  Zhang, M. et al. 2015. Stem Cells. 33: 1456-69.

PMID: # 25402622  Mao, F. et al. 2015. Hum. Mutat. 36: 240-9.

PMID: # 25709708  Wong, HS. et al. 2015. Evid Based Complement Alternat Med. 2015: 142059.

PMID: # 26247736  Su, X. et al. 2015. Cell death & disease. 6: e1851.

PMID: # 25944759  Choi, HS. et al. 2015. Molecular nutrition & food research. 59: 1458-71.

Citations 1 to 10 of 21 total

This AMPK inhibitor can be used in mice?

Asked by: Saroca
Thank you for your question. Unfortunately we are not able to provide that information. Our compounds are not pharmaceutical grade and not manufactured under GMP guidelines. Please consult your principal investigator and your animal care and use committee (ACUC) regarding the use of our compounds.
Answered by: Technical Support
Date published: 2019-01-17

I need it in a powder form 25grams bml 275 case 866 405 64 3 how much it will cost and I would like to order it

Asked by: Inpact
Please contact our Special Orders Department for bulk order pricing. Please call us toll-free at (800) 457-3801 option 2, or use email specialorders@scbt.com.
Answered by: Technical Support
Date published: 2018-11-19

What is the difference between sc-200689 and sc-361173?

Asked by: Io5ay
Thank you for your question. Our other product, sc-361173: BML-275 hydrochloride salt, is the hydrochloride salt form of BML-275.
Answered by: Technical Support
Date published: 2017-03-09

Can this product be dissolved in HCl?

Asked by: Io5ay
Thank you for your question. Yes, sc-200689 is soluble in 100mM HCl.
Answered by: Technical Support
Date published: 2017-03-09

What techniques will facilitate dissolving this product into solution, and is it soluble in DMSO?

Asked by: Io5ay
Thank you for your question. sc-200689: BML-275 is soluble in MeOH, DMSO or in 100mM HCl. This compound can be a bit tough to get into solution. Warming and vortexing certainly will not harm anything and we recommend using fresh completely anhydrous DMSO.
Answered by: Technical Support
Date published: 2018-11-15
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Rated 5 out of 5 by from Tang Tang, Q. et al. (PubMed 23541682) used product sc-200689 (BML-275, Compound C), a cell-permeable pyrazolopyrimidine derivative that inhibits AMP Kinase, to find that resveratrol-induced autophagy in ESCC cells is not mediated by the AMPK pathway. -SCBT Publication Review
Date published: 2015-01-03
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