1. Cell Cycle/DNA Damage Cytoskeleton Epigenetics
  2. Mitosis Kinesin Microtubule/Tubulin Aurora Kinase
  3. UMK57

UMK57 is a MCAK activator and kinetochore-microtubule destabilizer. UMK57 enhances MCAK-dependent microtubule depolymerization, increases kinetochore-microtubule turnover, reduces chromosome mis-segregation and lagging chromosomes, and inhibits cancer cell proliferation. UMK57 triggers adaptive resistance in Aurora B cancer cells via reversible Aurora B signaling pathway alterations. UMK57 can be used for the research of solid tumors.

For research use only. We do not sell to patients.

UMK57

UMK57 Chemical Structure

CAS No. : 342595-74-8

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Description

UMK57 is a MCAK activator and kinetochore-microtubule destabilizer. UMK57 enhances MCAK-dependent microtubule depolymerization, increases kinetochore-microtubule turnover, reduces chromosome mis-segregation and lagging chromosomes, and inhibits cancer cell proliferation. UMK57 triggers adaptive resistance in Aurora B cancer cells via reversible Aurora B signaling pathway alterations. UMK57 can be used for the research of solid tumors[1][2].

IC50 & Target[1]

Kif2c/MCAK

 

In Vitro

UMK57 (100 nM; 1-72 h) reduces anaphase lagging chromosome rates in SW620 cells acutely[1].
UMK57 (100 nM; 1-72 h) selectively increases the levels of Aurora kinase A and TPX2 on mitotic spindles without altering Aurora kinase A activation status in SW620 cells[1].
UMK57 specifically potentiates MCAK-mediated microtubule depolymerization in vitro without inhibiting kinesin ATPase activity[2].
UMK57 (0.1-50 μM; 3 days) inhibits U2OS cell proliferation in a dose-dependent manner[2].
UMK57 (100 nM; <1h) suppresses chromosome mis-segregation in U2OS, HeLa, and SW-620 CIN cancer cells[2].
UMK57 (100 nM; 1 h) reduces metaphase k-MT attachment stability in U2OS cells in an MCAK-dependent manner, with no effect on prometaphase k-MT stability initially, but induces reversible hyper-stabilization of prometaphase k-MTs after extended continuous treatment[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: U2OS cells
Concentration: 0.1; 0.5; 1; 5; 20; 50 μM
Incubation Time: 3 days
Result: Inhibited cell proliferation of U2OS cells in a dose-dependent manner.
Molecular Weight

295.40

Formula

C17H17N3S

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=CC=C(C=C1)C2=CSC3=NC=NC(N4CCCC4)=C32

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

Ethanol : 6.67 mg/mL (22.58 mM; Need ultrasonic)

DMSO : 2 mg/mL (6.77 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3852 mL 16.9262 mL 33.8524 mL
5 mM 0.6770 mL 3.3852 mL 6.7705 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 3.3852 mL 16.9262 mL 33.8524 mL 84.6310 mL
5 mM 0.6770 mL 3.3852 mL 6.7705 mL 16.9262 mL
Ethanol 10 mM 0.3385 mL 1.6926 mL 3.3852 mL 8.4631 mL
15 mM 0.2257 mL 1.1284 mL 2.2568 mL 5.6421 mL
20 mM 0.1693 mL 0.8463 mL 1.6926 mL 4.2316 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
UMK57
Cat. No.:
HY-122236
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