HY-124798

HY-124798

Identifiers
IUPAC name 4-bromo-6-(3,4-dichlorophenyl)sulfanyl-1-[[4-(dimethylcarbamoyl)phenyl]methyl]indole-2-carboxylic acid
CAS Number	2216763-38-9
PubChem CID	132281917
Chemical and physical data
Formula	C25H19BrCl2N2O3S
Molar mass	578.30 g·mol−1
3D model (JSmol)	Interactive image
SMILES CN(C)C(=O)C1=CC=C(C=C1)CN2C(=CC3=C2C=C(C=C3Br)SC4=CC(=C(C=C4)Cl)Cl)C(=O)O
InChI InChI=1S/C25H19BrCl2N2O3S/c1-29(2)24(31)15-5-3-14(4-6-15)13-30-22-11-17(34-16-7-8-20(27)21(28)10-16)9-19(26)18(22)12-23(30)25(32)33/h3-12H,13H2,1-2H3,(H,32,33) Key:MJYFVDNMTKLGTH-UHFFFAOYSA-N

HY-124798 (Rheb inhibitor NR1) is the first compound to be developed that acts as a potent and selective inhibitor of Rheb, a GTP-binding protein which acts as an endogenous activator of the mechanistic target of rapamycin (mTOR) subtype mTORC1. Since many of the side effects of rapamycin and its analogues are thought to result from binding to the other subtype mTORC2, it is hoped that selective inhibition of mTORC1 should have a more selective effects profile. As mTORC1 and mTORC2 have binding sites that are very similar in structure, it has been challenging to develop highly subtype selective inhibitors, making indirect inhibition via modulation of other messenger proteins such as Rheb an attractive approach. However, since HY-124798 has a relatively weak IC₅₀ of 2.1μM, and Rheb also has other targets in addition to mTORC1, it remains to be established whether it will deliver the hoped for improvements in pharmacological profile.

See also

• MB-3 (drug)