Alternate TextTo enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
Home > Products > Novel inhibitors

MN58b

  Cat. No.:  DC21335   Featured
Chemical Structure
203192-01-2
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
MN58b is a potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.4 uM, >30-fold selectivity over ChoKβ and does not affect MAPKs, PI3Ks, and other enzymes involved in the regulation of phospholipid metabolism.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 203192-01-2
Chemical Name: MN58b bromide
Synonyms: MN-58b;MN 58b
SMILES: C(C1=CC=C(C[NH0+]2C=CC(N(C)C)=CC=2)C=C1)CCCC1=CC=C(C[NH0+]2C=CC(N(C)C)=CC=2)C=C1.[BrH0-].[BrH0-]
Formula: C32H40Br2N4
M.Wt: 640.508
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity[1][2].
Target: Choline kinase α (CHKα)[1]
In Vivo: MN58b (4 mg/kg; intraperitoneal injection; once a day; for 5 days; MF-1 nude mice) treatment significantly decreases phosphomonoesters in both HT29 and MDA-MB-231 xenografts. Phosphocholine levels are found to correlate with choline kinase activities[2]. Animal Model: MF-1 nude mice with HT29 or MDA-MB-231 cells[2] Dosage: 4 mg/kg Administration: Intraperitoneal injection; once a day; for 5 days Result: Phosphomonoesters decreased significantly.
In Vitro: The IC50s of MN58b for parental and Gemcitabine-resistant Suit2 007 cells are 3.14 µM and 0.77 µM, respectively[1]. MN58b (1-5 µM; 72 hours; SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells) has a marked effect on colony formation at 1 µM, and growth is completely abolished at 5 µM in all the cell lines[1]. MN58b ((1-10 µM; 24-48 hours; SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells) induces apoptosis and this response correlates with CHKα expression[1]. Cell Viability Assay[1] Cell Line: SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells Concentration: 1 µM, 5 µM Incubation Time: 72 hours Result: Inhibited cells growth. Apoptosis Analysis[1] Cell Line: SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells Concentration: 1 µM, 2 µM, 5 µM, 10 µM Incubation Time: 24 and 48 hours Result: Induced cell apoptosis.
References: [1]. Mazarico JM, et al. Choline Kinase Alpha (CHKα) as a Therapeutic Target in Pancreatic Ductal Adenocarcinoma: Expression, Predictive Value, and Sensitivity to Inhibitors. Mol Cancer Ther. 2016 Feb;15(2):323-33. [2]. Al-Saffar NM, et al. Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models. Cancer Res. 2006 Jan 1;66(1):427-34.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC31074 Isopropyl myristate Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC75868 AZ14133346 AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865 TI17 ​​TI17​​ represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.
DC75816 Nisoxetine Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.
DC75641 GENZ-644282 TFA salt Genz-644282, also known as SAR402674, is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.
DC75325 PSMA-617 TFA PSMA-617, also know as vipivotide tetraxetan, is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA617 possesses a small peptide, which was designed to target prostate-specific membrane antigen (PSMA). PSMA617 demonstrates high radiolytic stability for at least 72 h. PSMA617 has high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined). 177 Lu-PSMA-617 offers a potential additional life-prolonging treatment option for men with mCRPC.
DC75202 Fosaprepitant free acid Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4
DC74748 O4I4 O4I4 (compound 23) is a OCT4-inducing compound with metabolical stability.
DC74684 ZH8667 ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.
DC74646 EB-PSMA-617 EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia