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Overview
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We have designed this kit to label any antibody (IgG type) with UM171 through a stable amide bond. The user provides the antibody, while the kit includes UM171 N-Hydroxysuccinimide (NHS) ester. This UM171-NHS ester couples directly to the antibody's surface amines in a single step. The final product is then purified to remove any unreacted UM171.
UM171 is a small molecule first discovered in Canada and published in 2014. It is known for its ability to enhance hemapoetic stem cell renewal (Fares I. et. al. Science 2014, 345, 1509-1512). UM171 activates the CULLIN3KBTBD4 ubiquitin ligase, which specifically targets the LSD1-CoREST repressor complex for proteasomal degradation (Chagraoui J. et al. Cell Stem Cell. 2021, 28, 48-62). A phase 1-2 trial of UM171-expanded cord blood (CB) transplants demonstrated safety andd favorable preliminary efficacy.
This kit provides materials to conjugate 1 to 3 mg of one (1) antibody sample (CM11433x1) or three (3) antibody samples (CM11433x3) of IgG with UM171 via a stable amide bond.
Drug Information
Name: UM171
Synonym: 4-N-[2-benzyl-7-(2-methyltetrazol-5-yl)-9H-pyrimidio[4,5-b]indol-4-yl]cyclohexane-1,4-diamine, trans-N1-(7-(2-Methyl-2H-tetrazol-5-yl)-2-(phenylmethyl)-9H-pyrimido(4,5-b)indol-4-yl-cyclohexanediamine.
CAS number: 1448724-09-1
Mechanism of action (list only few): Activates the CULLIN3KBTBD4 ubiquitin ligase, which specifically targets the LSD1-CoREST repressor complex for proteasomal degradation.
Medical usage: Enhance hematopoietic stem cell renewal.
Requirement for Antibody
Preferably >90% pure by gel electrophoresis
Total amount: 1-3 mg of protein content as measured by UV. Note: The accuracy of your protein measurement is the single most important factor in obtaining an optimized DAR of 4. The user manual contains instructions for measuring protein amount under the "Other Considerations" section.
Key Features of this PerKit™
• Provides a simple and efficient method to label IgG with UM171
• Ensures a stable linkage
• Quick and easy preparation: 4 h process with less than 1 hour of hands-on time
• Includes all necessary reagents and supplies for both preparation and purification
• Optimized Drug-to-Antibody Ratio (DAR): Average 3-5 UM171 molecules per antibody
• Features a stabilizing buffer for long-term storage.
• Delivers >99% of conjugated products, free of unreacted UM171
• Options to choose tailored services after conjugationPlease contact us at for specific academic pricing.
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- Properties
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Overview