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MedKoo Cat#: 532466 | Name: PF-4800567
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

PF-4800567
PF-4800567
CAS#1188296-52-7 (free base)

Theoretical Analysis

MedKoo Cat#: 532466

Name: PF-4800567

CAS#: 1188296-52-7 (free base)

Chemical Formula: C17H18ClN5O2

Exact Mass: 359.1149

Molecular Weight: 359.81

Elemental Analysis: C, 56.75; H, 5.04; Cl, 9.85; N, 19.46; O, 8.89

Price and Availability

Size Price Availability Quantity
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,350.00 2 Weeks
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Related CAS #
1188296-52-7 (free base) 1391052-28-0 (HCl)
Synonym
PF-4800567; PF 4800567; PF4800567;
IUPAC/Chemical Name
3-[(3-chlorophenoxy)methyl]-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine
InChi Key
AUMDBEHGJRZSOO-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H18ClN5O2/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)
SMILES Code
NC1=C2C(N(C3CCOCC3)N=C2COC4=CC=CC(Cl)=C4)=NC=N1
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
>2 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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM.
In vitro activity:
To test this, this study characterized 3-(3-chloro-phenoxymethyl)-1-(tetrahydro-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine (PF-4800567), a novel and potent inhibitor of CK1epsilon (IC(50) = 32 nM) with greater than 20-fold selectivity over CK1delta. PF-4800567 completely blocks CK1epsilon-mediated PER3 nuclear localization and PER2 degradation. Reference: J Pharmacol Exp Ther. 2009 Aug;330(2):430-9. https://pubmed.ncbi.nlm.nih.gov/19458106/
In vivo activity:
TBD
Solvent mg/mL mM comments
Solubility
DMF 25.0 69.48
DMF:PBS (pH 7.2) (1:1) 0.5 1.39
DMSO 52.3 145.45
Ethanol 1.0 2.78
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 359.81 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.

Recalculate based on batch purity %
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:
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.
In vitro protocol:
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.
In vivo protocol:
TBD
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.