Rapamycin

Inhibits mTOR (FRAP domain) as a complex with FKBP12 of MTOR

Structure

Information

Protein target names: MTOR

Mechanism of action: Inhibits mTOR (FRAP domain) as a complex with FKBP12

Recommended in-cell concentration:
1 nM - 200 nM
Primary References:

In Vitro Validations

Uniprot ID: P42345
Target Class: Kinase
Target SubClass: Atypical
Potency: Ki
Potency Value: 0.2 nM (FKBP1A)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Serine/threonine-protein kinase mTOR, RAPT1, RAFT1 ...

DOI Reference: 10.1038/369756a0

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 14 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

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).

(last updated: 20 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 1 Sept 2016 )