PP242 Inhibitor CAS No. 1092351-67-1

Cat. No.	Name	Size	Price
KI0549	PP242	10 mg	$370
	PP242	25 mg	$616
	PP242	100 mg	$1012

Chemical Characteristic

Product Name	PP242
CAS No.	1092351-67-1
Molecular Weight	308.34
Formula	C₁₆H₁₆N₆O
Chemical Name	2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
Smiles	[nH]1c(cc2cc(ccc12)O)c1c2c(ncnc2N)n(n1)C(C)C
Chemical Structure

Biological activities

PP242 is a mammalian target of rapamycin (mTOR) inhibitor. The IC50 of PP242 is 13.7, 24.7 and 40 nM against recombinant mTOR, mTORC1 complex and Hela cells with mTOR, respectively. 10 μM PP242 reveals strong (90%) inhibition of a number of kinases in the tyrosine kinase family/TK (including BTK, Eph, FGF receptor), calcium/calmodulin-dependent protein kinase family/CAMK (BRSK2, CHK2, and MLCK), CMGC family (DYK2/3, HIPK2 CDK, MAPK, GSK3, CLK, and ERK8), casein kinase family (CK1δ), and AGC family (PKCα). PP242 exhibits potent protection of all PIKK family members (ATM, ATR, PI3Ks, DNA-PK, and SMG1), lipid kinase (PIP5K3), as well as some protein kinases in the CMGC, AGC, and STE families. In addition, PP242 efficiently inhibits the RET receptor and JAK1/2/3 kinases with EC50 of 42 nM and 0.780 μM. ^[1] PP242 strongly suppresses both mTORC1 and mTORC2-mediated activities and exerts potent cytotoxicity against leukemia cells. PP242 dose-dependently increases the proportion of Annexin V positive apoptotic cells. PP242 inhibits HEL and SET2 cells with 0.172 nM and 0.062 nM, respectively.^[2] PP242 inhibits 4E-BP1 phosphorylation.^[3] PP242 induces ERK activation in MM cell lines as well as primary cells.^[4] PP242 causes death of mouse and human leukemia cells.^[5] PP242 increases MAPK phosphorylation. ^[6] In vivo, PP242 delays leukemia onset and augments the effects of the current front-line tyrosine kinase inhibitors more effectively than does rapamycin.^[5]

Protocols

PP242 is dissolved in PEG 300.^[6]

References

[1] Liu Q, et al. Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. J Biol Chem. 2012, 287(13): 9742-9752. [2] Bogani C, et al. mTOR inhibitors alone and in combination with JAK2 inhibitors effectively inhibit cells of myeloproliferative neoplasms. PLoS One. 2013, 8(1): e54826. [3] Ducker GS, et al. Incomplete inhibition of phosphorylation of 4E-BP1 as a mechanism of primary resistance to ATP-competitive mTOR inhibitors. Oncogene. 2013. [4] Hoang B, et al. The PP242 mammalian target of rapamycin (mTOR) inhibitor activates extracellular signal-regulated kinase (ERK) in multiple myeloma cells via a target of rapamycin complex 1 (TORC1)/eukaryotic translation initiation factor 4E (eIF-4E)/RAF pathway and activation is a mechanism of resistance. J Biol Chem. 2012, 287(26): 21796-21805. [5] Janes MR, et al. Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat Med. 2010, 16(2): 205-213. [6] Dormond-Meuwly A, et al. The inhibition of MAPK potentiates the anti-angiogenic efficacy of mTOR inhibitors. Biochem Biophys Res Commun. 2011, 407(4): 714-719.

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