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HMN-214 - 10mM in DMSO, high purity , CAS No.173529-46-9(DMSO)

    Grade & Purity:
  • 10mM in DMSO
In stock
Item Number
H409194
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Availability
Price Qty
H409194-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$302.90

PLK1 Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms Acetamide, N-[(4-methoxyphenyl)sulfonyl]-N-[2-[(1E)-2-(1-oxido-4-pyridinyl)ethenyl]phenyl]-
Specifications & Purity 10mM in DMSO
Biochemical and Physiological Mechanisms HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
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Product Description

Information

HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
In vitro

HMN-214 is an oral prodrug that is rapidly converted to HMN-176. The in vitro data of HMN-214 are scarce. However, HMN-176, active metabolite of HMN-214, shows potent and broad-spectrumanti-tumor activity against various cancer cells, including HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr, with a mean IC50 value of 118 nM. HMN-176 is also cytotoxic to drug-resistant human and murine cell lines, including P388/CDDP, P388/VCR, K2/CDDP, and K2/VP-16, with IC50 values ranging from 143 nM–265 nM. In HeLa cells, HMN-176 (3 μM) blocks cell cycle at G2/M phase. In Doxorubicin-resistant K2/ARS cells, HMN-176 inhibits cell growth with an IC50 value of 2 μM. HMN-176 (3 μM) down-regulates the expression of the multidrug resistance gene (MDR1), due to the disturbance of NF-Y transcription factor binding to the MDR1 promoter. In human RPE1 and CFPAC-1 cells, HMN-176 (2.5 μM) delays satisfaction of the spindle assembly checkpoint. HMN-176 (250 nM–2.5 μM) inhibits meiotic spindle assembly and aster formationin Spisula oocytes. HMN-176 (2.5 μM) also inhibits aster microtubule formation from human centrosomes. These results indicate that the anti-tumor activity of HMN-176 is at least partially via disrupting centrosome-mediated MT assembly during mitosis.

In vivo

HMN-214 is an oral pro-drug of HMN-176 with improved oral absorption. HMN-214 (30 mg/kg) triggers no obvious neurotoxicity in mice. In mouse xenograft model of PC-3, A549, and WiDr cells, HMN-214 (10 mg/kg–20 mg/kg) inhibits tumor growth. In nude mice model bearing multidrug-resistant KB-A.1 cells, HMN-214 (10 mg/kg–20 mg/kg) significantly suppresses MDR1 mRNA expression.
Cell Data

cell lines:

Concentrations:0–10 μM, dissolved in DMSO

Incubation Time:72 hours

Powder Purity:≥99%

Names and Identifiers

Smiles COC1=CC=C(C=C1)[S](=O)(=O)N(C(C)=O)C2=C(C=CC=C2)\C=C\C3=CC=[N+]([O-])C=C3
Molecular Weight 424.47

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 24 mg/mL (99.3 mM); Ethanol: 2 mg/mL (8.27 mM); Water: Insoluble;

Solution Calculators

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