2. Metabolic Enzyme/Protease Apoptosis
  3. E1/E2/E3 Enzyme Apoptosis
  4. UC-764864

UC-764864 is a selective UBE2N inhibitor. UC-764864 covalently binds UBE2N catalytic Cys87, blocks ubiquitin-UBE2N thioester formation and polyubiquitin chain synthesis. UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates, and induces cell apoptosis. UC-764864 can be used for the research of acute myeloid leukemia.

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

UC-764864

UC-764864 Chemical Structure

CAS No. : 278806-03-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

UC-764864 is a selective UBE2N inhibitor. UC-764864 covalently binds UBE2N catalytic Cys87, blocks ubiquitin-UBE2N thioester formation and polyubiquitin chain synthesis. UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates, and induces cell apoptosis. UC-764864 can be used for the research of acute myeloid leukemia[1].

In Vitro

UC-764864 (1-10 μM) potently and selectively inhibits wild-type UBE2N catalytic activity via its Cys87 residue[1].
UC-764864 (1 nM-0.1 mM; 1 h) selectively binds to the catalytic Cys87 residue of UBE2N in human MOLM-13 AML cells[1].
UC-764864 (2 μM; 24 h) selectively reduces UBE2N autoubiquitination at Lys92 and disrupts UBE2N-dependent innate immune and inflammatory signaling pathways in human MOLM-13 AML cells[1].
UC-764864 (1 nM-0.1 mM) potently and selectively inhibits UBE2N-mediated NF-κB activity downstream of multiple innate immune receptors in human THP-1 AML cells, with no effect on UBE2N-independent pathways[1].
UC-764864 (0-10 μM; 24-72 h) selectively suppresses viability and clonogenic potential of human AML cell lines and MDS cells in vitro, with no effect on healthy cord blood CD34+ cells[1].
UC-764864 (0.5-5 μM; 24-96 h) induces time- and dose-dependent cell death and apoptosis in human MOLM-13 AML cells in vitro[1].
UC-764864 (100 nM-10 μM; 72 h) exerts inhibitory effects on human MOLM-13 AML cell viability that depend on targeting the catalytic Cys87 residue of UBE2N, as UBE2NC87S-expressing cells are resistant to UC-764864[1].

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

UC-764864 Related Antibodies

Cell Viability Assay[1]

Cell Line: human MOLM-13 AML cells
Concentration: 0.5 μM; 1 μM; 2μM
Incubation Time: 24 h
Result: Increased the proportion of apoptotic cells from ~15% to ~35% (P < 0.01) after 24-hour treatment with 2 μM.
Molecular Weight

322.42

Formula

C19H18N2OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(CC)C=C1)/C=C/SC2=NC3=C(N2)C=CC(C)=C3
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: 

DMSO : 125 mg/mL (387.69 mM; Need ultrasonic; 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 3.1015 mL 15.5077 mL 31.0154 mL
5 mM 0.6203 mL 3.1015 mL 6.2031 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 1 mM 3.1015 mL 15.5077 mL 31.0154 mL 77.5386 mL
5 mM 0.6203 mL 3.1015 mL 6.2031 mL 15.5077 mL
10 mM 0.3102 mL 1.5508 mL 3.1015 mL 7.7539 mL
15 mM 0.2068 mL 1.0338 mL 2.0677 mL 5.1692 mL
20 mM 0.1551 mL 0.7754 mL 1.5508 mL 3.8769 mL
25 mM 0.1241 mL 0.6203 mL 1.2406 mL 3.1015 mL
30 mM 0.1034 mL 0.5169 mL 1.0338 mL 2.5846 mL
40 mM 0.0775 mL 0.3877 mL 0.7754 mL 1.9385 mL
50 mM 0.0620 mL 0.3102 mL 0.6203 mL 1.5508 mL
60 mM 0.0517 mL 0.2585 mL 0.5169 mL 1.2923 mL
80 mM 0.0388 mL 0.1938 mL 0.3877 mL 0.9692 mL
100 mM 0.0310 mL 0.1551 mL 0.3102 mL 0.7754 mL
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Help & FAQs
  • 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.

Keywords:

UC-764864278806-03-4UC764864UC 764864E1/E2/E3 EnzymeApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasepolyubiquitin chain synthesisMOLM-13 AML cellsacute myeloid leukemiaCys87CD34+ cellsTHP-1 AML cellsubiquitinhematopoietic stem and progenitor cellsUBE2NNF-κBInhibitorinhibitorinhibit

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