Rapamycin

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InChi Key:

QFJCIRLUMZQUOT-HPLJOQBZSA-N

PAINs evaluation:

PAINs free

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

0.2 nM (FKBP1A)

In cell validation

On target activity in cells

Potency in cells:

IC50

0.1 nM

Potency assay (cells):

Inhibition of G1 progression in MG-63 cells

Primary Reference

Reference (doi):

Nature J Biol Chem

Reference (PMID):

8008069 9933627

SAB Rating

Rating for use in Cells

3 review(s)

Rating for use in Model Organisms

3 review(s)

SAB Members

SAB Comments

Rapamycin (also known as sirolimus) is a well established Mammalian Target of Rapamycin (mTOR; FRAP1) Inhibitor. Other validated mechanisms of action include cytochrome P450 (various isoforms) inhibition and P-glycoprotein (MDR-1; ABCB1) inhibition. Rapamycin is a naturally occurring macrolide produced by the bacterium Streptomyces hygroscopicus. Several semisynthetic 'rapalogs' have been generated which alter key pharmaceutical properties of the probe. These agents include everolimus, ridaforolimus and temsirolimus. Rapamycin and the rapalogs are wonderful agents for interrogating Mammalian Target of Rapamycin (mTOR; FRAP1) and can ideally be used alongside synthetic inhibitors (such as Vistusertib) which often target both the mTORC1 and mTORC2 complex (as well as the phosphatidylinositol 3-kinase (PI3K) enzyme class).

Rapamycin

Probe Availability

Probe Information

Target Details

FRAP, FRAP1, FRAP2, RAFT1, RAPT1, SKS

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

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Rapamycin

Probe Availability

Probe Information

Target Details

FRAP, FRAP1, FRAP2, RAFT1, RAPT1, SKS

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?