1H-Pyrrole-2-carboxylic acid, 3-(5-chloro-1H-indol-4-yl)-5-(1H-indol-4-yl)-4-(1-methylethyl)- Chemical Properties

Boiling point:

717.4±60.0 °C(Predicted)

Density 

1.403±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

pka

4.11±0.50(Predicted)

form 

Solid

color 

White to light yellow

1H-Pyrrole-2-carboxylic acid, 3-(5-chloro-1H-indol-4-yl)-5-(1H-indol-4-yl)-4-(1-methylethyl)- Usage And Synthesis

Biological Activity

RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM[1]. RB-3 decreases the global level of H2A ubiquitination and induces differentiation in leukemia cell lines and primary acute myeloid leukemia (AML) samples[1].RB-3 inhibits H2A ubiquitination with an IC50 of 1.6 μM[1].RB-3 inhibits PRC1 and disrupts the interaction with nucleosomes[1].RB-3 reduces colony formation in a mixed lineage leukemia (MLL)-eleven nineteen leukemia (ENL) model[1].

References

[1]. Shirish Shukla, et al. Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain. Nat Chem Biol. 2021 Jul;17(7):784-793.