RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5[1].
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity[1]. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α[2]. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity[3].