Description
DJ001 (2161306-12-8) is a potent and specific inhibitor of receptor type protein tyrosine phosphatase-sigma (PTPσ) IC50=1.54 μM and >10 μM for 20 other phosphatases.1 Promotes hematopoietic stem cell regeneration in vivo. In mice treated with 5-fluorouracil or irradiated, DJ001 promoted HSC regeneration accelerated hematologic recovery and improved survival. The mode of inhibition of PTPs is via non-competitive allosteric binding. Suppression of radiation-induced HSC apoptosis occurs via activation of Rho GTPase, Rac1 and induction of BCL-XL. Treatment of irradiated human HSCs with DJ001 promotes the regeneration of human HSCs capable of multilineage in vivo repopulation.1
Uses
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration[1].
in vivo
DJ001 (5mg/kg; subcutaneous injection; for 24 hours; female C57BL/6 mice) significantly decreases the percentage of apoptotic BM KSL cells in C57BL/6 mice at 24h following 500cGy TBI. DJ001 suppresses radiation-induced HSC apoptosis via activation of the RhoGTPase, RAC1, and induction of BCL-XL[1].
| Animal Model: | Female C57BL/6 mice (8-10-week-old) irradiated with total body irradiation (TBI)[1] |
| Dosage: | 5mg/kg |
| Administration: | Subcutaneous injection; for 24 hours |
| Result: | Significantly decreased the percentage of apoptotic BM KSL cells in C57BL/6 mice at 24h following 500cGy TBI.
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References
References/Citations:
1.Zhang et al. (2019), PTPσ inhibitors promote hematopoietic stem cell regeneration; Nat. Commun., 10 3667
