XRK3F2 | p62 Inhibitor

MedKoo Cat#: 558760 | Name: XRK3F2

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Description:

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

XRK3F2 is an inhibitor of signaling via the ZZ domain of p62 (Sequestosome 1), blocking tumor necrosis factor (TNF) and multiple myeloma‐induced Gfi1 upregulation, resulting in decreased binding and recruitment of HDAC1 to the RUNX2 promoter in pre‐OBs.

Chemical Structure

XRK3F2

CAS#NONE

Theoretical Analysis

MedKoo Cat#: 558760

Name: XRK3F2

CAS#: NONE

Chemical Formula: C23H24ClF2NO3

Exact Mass: 0.0000

Molecular Weight: 435.90

Elemental Analysis: C, 63.38; H, 5.55; Cl, 8.13; F, 8.72; N, 3.21; O, 11.01

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 280.00
10mg	USD 440.00
50mg	USD 970.00

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Related CAS #

No Data

Synonym

XRK-3F2; XRK 3F2; XRK3F2

IUPAC/Chemical Name

2-[[3,4-Bis[(4-fluorophenyl)methoxy]phenyl]methylamino]ethanol hydrochloride

InChi Key

XBSQIUHKVROJDN-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H23F2NO3.ClH/c1-26(12-13-27)21-10-11-22(28-15-17-2-6-19(24)7-3-17)23(14-21)29-16-18-4-8-20(25)9-5-18;/h2-11,14,27H,12-13,15-16H2,1H3;1H

SMILES Code

CN(CCO)C1=CC=C(OCC2=CC=C(F)C=C2)C(OCC3=CC=C(F)C=C3)=C1.[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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 435.90 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

1: Alcober-Boquet L, Zang T, Pietsch L, Suess E, Hartmann M, Proschak E, Gross LZF, Sacerdoti M, Zeuzem S, Rogov VV, Leroux AE, Piiper A, Biondi RM. The PB1 and the ZZ domain of the autophagy receptor p62/SQSTM1 regulate the interaction of p62/SQSTM1 with the autophagosome protein LC3B. Protein Sci. 2024 Jan;33(1):e4840. doi: 10.1002/pro.4840. PMID: 37984441; PMCID: PMC10751729. 2: Marino S, Petrusca DN, Bishop RT, Anderson JL, Sabol HM, Ashby C, Layer JH, Cesarano A, Davé UP, Perna F, Delgado-Calle J, Chirgwin JM, Roodman GD. Pharmacologic targeting of the p62 ZZ domain enhances both anti-tumor and bone- anabolic effects of bortezomib in multiple myeloma. Haematologica. 2024 May 1;109(5):1501-1513. doi: 10.3324/haematol.2023.283787. PMID: 37981834; PMCID: PMC11063840. 3: Chen S, Wang X, Liu Z, Wang J, Guo Y, Wang Q, Huang H, Li Y, Yu C, Xu C. Olfactomedin 4 deletion exacerbates nonalcoholic fatty liver disease through P62-dependent mitophagy in mice. Metabolism. 2023 Nov;148:155679. doi: 10.1016/j.metabol.2023.155679. Epub 2023 Aug 21. PMID: 37611821. 4: Zhang L, Fang Y, Cheng X, Lian Y, Xu H. Interaction between TRPML1 and p62 in Regulating Autophagosome-Lysosome Fusion and Impeding Neuroaxonal Dystrophy in Alzheimer's Disease. Oxid Med Cell Longev. 2022 Jan 25;2022:8096009. doi: 10.1155/2022/8096009. PMID: 35116093; PMCID: PMC8807035. 5: Li Y, Li Y, Yin J, Wang C, Yang M, Gu J, He M, Xu H, Fu W, Zhang W, Ru Y, Liu X, Li Y, Xin Y, Gao H, Xie X, Gao Y. A mitophagy inhibitor targeting p62 attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Lett. 2021 Jul 10;510:24-36. doi: 10.1016/j.canlet.2021.04.003. Epub 2021 Apr 13. PMID: 33862150. 6: Wang T, Zhao N, Peng L, Li Y, Huang X, Zhu J, Chen Y, Yu S, Zhao Y. DJ-1 Regulates Microglial Polarization Through P62-Mediated TRAF6/IRF5 Signaling in Cerebral Ischemia-Reperfusion. Front Cell Dev Biol. 2020 Dec 17;8:593890. doi: 10.3389/fcell.2020.593890. PMID: 33392187; PMCID: PMC7773790. 7: Adamik J, Silbermann R, Marino S, Sun Q, Anderson JL, Zhou D, Xie XQ, Roodman GD, Galson DL. XRK3F2 Inhibition of p62-ZZ Domain Signaling Rescues Myeloma- Induced GFI1-Driven Epigenetic Repression of the Runx2 Gene in Pre- osteoblasts to Overcome Differentiation Suppression. Front Endocrinol (Lausanne). 2018 Jun 29;9:344. doi: 10.3389/fendo.2018.00344. PMID: 30008697; PMCID: PMC6033965. 8: Teramachi J, Silbermann R, Yang P, Zhao W, Mohammad KS, Guo J, Anderson JL, Zhou D, Feng R, Myint KZ, Maertz N, Beumer JH, Eiseman JL, Windle JJ, Xie XQ, Roodman GD, Kurihara N. Blocking the ZZ domain of sequestosome1/p62 suppresses myeloma growth and osteoclast formation in vitro and induces dramatic bone formation in myeloma-bearing bones in vivo. Leukemia. 2016 Feb;30(2):390-8. doi: 10.1038/leu.2015.229. Epub 2015 Aug 19. PMID: 26286116; PMCID: PMC4740189.