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MedKoo Cat#: 407418 | Name: TP-064
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Description:

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

TP-064 is a potent and selective PRMT4 inhibitor. The in vitro activity of TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, TP-064 inhibits the methylation of MED12 with IC50 = 43 nM.

Chemical Structure

TP-064
TP-064
CAS#2080306-20-1

Theoretical Analysis

MedKoo Cat#: 407418

Name: TP-064

CAS#: 2080306-20-1

Chemical Formula: C28H34N4O2

Exact Mass: 458.2682

Molecular Weight: 458.61

Elemental Analysis: C, 73.33; H, 7.47; N, 12.22; O, 6.98

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
100mg USD 750.00 2 Weeks
1g USD 2,650.00 2 Weeks
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Related CAS #
No Data
Synonym
TP-064; TP 064; TP064.
IUPAC/Chemical Name
N-Methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide
InChi Key
VUIITYLFSAXKIQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H34N4O2/c1-29-15-18-32-16-12-23(13-17-32)27-19-22(11-14-30-27)21-31(2)28(33)24-7-6-10-26(20-24)34-25-8-4-3-5-9-25/h3-11,14,19-20,23,29H,12-13,15-18,21H2,1-2H3
SMILES Code
O=C(N(C)CC1=CC(C2CCN(CCNC)CC2)=NC=C1)C3=CC=CC(OC4=CC=CC=C4)=C3
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

Preparing Stock Solutions

The following data is based on the product molecular weight 458.61 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
1: Zhang Y, de Boer M, van der Wel EJ, Van Eck M, Hoekstra M. PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. Biochim Biophys Acta Mol Basis Dis. 2021 Nov 1;1867(11):166212. doi: 10.1016/j.bbadis.2021.166212. Epub 2021 Jul 24. PMID: 34311083. 2: Nakayama K, Szewczyk MM, Dela Sena C, Wu H, Dong A, Zeng H, Li F, de Freitas RF, Eram MS, Schapira M, Baba Y, Kunitomo M, Cary DR, Tawada M, Ohashi A, Imaeda Y, Saikatendu KS, Grimshaw CE, Vedadi M, Arrowsmith CH, Barsyte-Lovejoy D, Kiba A, Tomita D, Brown PJ. TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma. Oncotarget. 2018 Apr 6;9(26):18480-18493. doi: 10.18632/oncotarget.24883. PMID: 29719619; PMCID: PMC5915086. 3: Zhang Y, Verwilligen RAF, de Boer M, Sijsenaar TJP, Van Eck M, Hoekstra M. PRMT4 inhibitor TP-064 impacts both inflammatory and metabolic processes without changing the susceptibility for early atherosclerotic lesions in male apolipoprotein E knockout mice. Atherosclerosis. 2021 Dec;338:23-29. doi: 10.1016/j.atherosclerosis.2021.11.001. Epub 2021 Nov 8. PMID: 34785428. 4: Inoue F, Sone K, Toyohara Y, Tanimoto S, Takahashi Y, Kusakabe M, Kukita A, Honjoh H, Nishijima A, Taguchi A, Miyamoto Y, Tanikawa M, Iriyama T, Uchino MM, Tsuruga T, Wada-Hiraike O, Oda K, Osuga Y. Histone arginine methyltransferase CARM1 selective inhibitor TP-064 induces apoptosis in endometrial cancer. Biochem Biophys Res Commun. 2022 Apr 23;601:123-128. doi: 10.1016/j.bbrc.2022.02.086. Epub 2022 Feb 23. PMID: 35245741. 5: Xie H, Bacabac MS, Ma M, Kim EJ, Wang Y, Wu W, Li L, Xu W, Tang W. Development of Potent and Selective Coactivator-Associated Arginine Methyltransferase 1 (CARM1) Degraders. J Med Chem. 2023 Sep 28;66(18):13028-13042. doi: 10.1021/acs.jmedchem.3c00982. Epub 2023 Sep 13. PMID: 37703322; PMCID: PMC10775954. 6: Peng BL, Ran T, Chen X, Ding JC, Wang ZR, Li WJ, Liu W. A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo. J Med Chem. 2024 May 23;67(10):7921-7934. doi: 10.1021/acs.jmedchem.3c02315. Epub 2024 May 7. PMID: 38713486; PMCID: PMC11129188.