Rapamycin

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

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

MTOR

Inhibits mTOR (FRAP domain) as a complex with FKBP12

1 nM - 200 nM

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Probe Availability:

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

SERP 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 )