WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H531335
CAS#: 1391052-28-0 (HCl)
Description: PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ. PF4800567 significantly increased the amplitude of NMDAR-EPSCs and puff NMDA currents in PVN neurons in WKY rats but not in SHRs. PF4800567 caused an NMDAR-dependent increase in the excitability of PVN neurons only in WKY rats. Also, the CK1ε protein level in the PVN was significantly lower in SHRs than in WKY rats. Furthermore, intracerebroventricular infusion of PF4800567 increased blood pressure and lumbar sympathetic nerve activity in WKY rats, and this effect was eliminated by microinjection of the NMDAR antagonist into the PVN.
Hodoodo Cat#: H531335
Name: PF-4800567 hydrochloride
CAS#: 1391052-28-0 (HCl)
Chemical Formula: C17H19Cl2N5O2
Exact Mass: 395.09
Molecular Weight: 396.272
Elemental Analysis: C, 51.53; H, 4.83; Cl, 17.89; N, 17.67; O, 8.07
Related CAS #: 1188296-52-7 (free base) 1391052-28-0 (HCl)
Synonym: PF-4800567 hydrochloride; PF-4800567; PF 4800567; PF4800567;
IUPAC/Chemical Name: 3-[(3-Chlorophenoxy)methyl]-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine hydrochloride
InChi Key: QZXZQMUZEHTFHD-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H18ClN5O2.ClH/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12;/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21);1H
SMILES Code: NC1=C2C(N(C3CCOCC3)N=C2COC4=CC=CC(Cl)=C4)=NC=N1.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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| In vitro activity: | |
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The following data is based on the product molecular weight 396.27 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Varghese RT, Young S, Pham L, Liang Y, Pridham KJ, Guo S, Murphy S, Kelly DF, Sheng Z. Casein Kinase 1 Epsilon Regulates Glioblastoma Cell Survival. Sci Rep. 2018 Sep 11;8(1):13621. doi: 10.1038/s41598-018-31864-x. PMID: 30206363; PMCID: PMC6134061.
2: Jayakumar AR, Tong XY, Shamaladevi N, Barcelona S, Gaidosh G, Agarwal A, Norenberg MD. Defective synthesis and release of astrocytic thrombospondin-1 mediates the neuronal TDP-43 proteinopathy, resulting in defects in neuronal integrity associated with chronic traumatic encephalopathy: in vitro studies. J Neurochem. 2017 Feb;140(4):645-661. doi: 10.1111/jnc.13867. Epub 2017 Jan 10. PMID: 27735996.
3: Patton AP, Chesham JE, Hastings MH. Combined Pharmacological and Genetic Manipulations Unlock Unprecedented Temporal Elasticity and Reveal Phase-Specific Modulation of the Molecular Circadian Clock of the Mouse Suprachiasmatic Nucleus. J Neurosci. 2016 Sep 7;36(36):9326-41. doi: 10.1523/JNEUROSCI.0958-16.2016. PMID: 27605609; PMCID: PMC5013184.
4: He TY, Wu DW, Lin PL, Wang L, Huang CC, Chou MC, Lee H. DDX3 promotes tumor invasion in colorectal cancer via the CK1ε/Dvl2 axis. Sci Rep. 2016 Feb 19;6:21483. doi: 10.1038/srep21483. PMID: 26892600; PMCID: PMC4759588.
5: Li DP, Zhou JJ, Pan HL. Endogenous casein kinase-1 modulates NMDA receptor activity of hypothalamic presympathetic neurons and sympathetic outflow in hypertension. J Physiol. 2015 Oct 1;593(19):4439-52. doi: 10.1113/JP270831. Epub 2015 Aug 18. PMID: 26174743; PMCID: PMC4594242.
6: Zhang L, Hastings MH, Green EW, Tauber E, Sladek M, Webster SG, Kyriacou CP, Wilcockson DC. Dissociation of circadian and circatidal timekeeping in the marine crustacean Eurydice pulchra. Curr Biol. 2013 Oct 7;23(19):1863-73. doi: 10.1016/j.cub.2013.08.038. Epub 2013 Sep 26. PMID: 24076244; PMCID: PMC3793863.
7: Smadja Storz S, Tovin A, Mracek P, Alon S, Foulkes NS, Gothilf Y. Casein kinase 1δ activity: a key element in the zebrafish circadian timing system. PLoS One. 2013;8(1):e54189. doi: 10.1371/journal.pone.0054189. Epub 2013 Jan 21. PMID: 23349822; PMCID: PMC3549995.
8: Long AM, Zhao H, Huang X. Structural basis for the potent and selective inhibition of casein kinase 1 epsilon. J Med Chem. 2012 Nov 26;55(22):10307-11. doi: 10.1021/jm301336n. Epub 2012 Nov 9. PMID: 23106386.
9: Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, Bolivar VJ, Loudon AS, Vitaterna MH, Turek FW, Palmer AA. Csnk1e is a genetic regulator of sensitivity to psychostimulants and opioids. Neuropsychopharmacology. 2012 Mar;37(4):1026-35. doi: 10.1038/npp.2011.287. Epub 2011 Nov 16. PMID: 22089318; PMCID: PMC3280656.
10: Cheong JK, Nguyen TH, Wang H, Tan P, Voorhoeve PM, Lee SH, Virshup DM. IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ɛ and Wnt/β-catenin independent inhibition of mitotic spindle formation. Oncogene. 2011 Jun 2;30(22):2558-69. doi: 10.1038/onc.2010.627. Epub 2011 Jan 24. PMID: 21258417; PMCID: PMC3109269.
11: Meng QJ, Maywood ES, Bechtold DA, Lu WQ, Li J, Gibbs JE, Dupré SM, Chesham JE, Rajamohan F, Knafels J, Sneed B, Zawadzke LE, Ohren JF, Walton KM, Wager TT, Hastings MH, Loudon AS. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15240-5. doi: 10.1073/pnas.1005101107. Epub 2010 Aug 9. PMID: 20696890; PMCID: PMC2930590.
12: Walton KM, Fisher K, Rubitski D, Marconi M, Meng QJ, Sládek M, Adams J, Bass M, Chandrasekaran R, Butler T, Griffor M, Rajamohan F, Serpa M, Chen Y, Claffey M, Hastings M, Loudon A, Maywood E, Ohren J, Doran A, Wager TT. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9. doi: 10.1124/jpet.109.151415. Epub 2009 May 19. PMID: 19458106.
