Stemregenin 1 (GMP)

Stemregenin 1 (SR1) (GMP) is a GMP-grade Stemregenin 1 (HY-15001). GMP-grade small molecules can be used as adjuvants in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with an IC₅₀ of 127 nM. Stemregenin 1 (GMP) can competitively bind to AhR and inhibit its nuclear translocation, inhibiting osteoclastogenesis and promoting hematopoietic progenitor cell expansion by blocking the AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway. Stemregenin 1 (GMP) can be used for the treatment of osteoporosis, in vitro expansion of hematopoietic stem cells, and the study of the mechanism of bone metabolic diseases^[1][2][3][4]. IC50 & Target:IC50: 127 nM (AhR)^[4] In Vitro:Stemregenin 1 (GMP) (1, 5, 10 μM; 7 days) promotes CD34+ cell expansion and enhance colony formation ability in human embryonic stem cell-derived hematopoietic progenitor cell experiments in a concentration-dependent manner, but inhibits cell proliferation at 10 μM^[1].
Stemregenin 1 (GMP) (0.75 μM; 7 days) combined with DMOG increases the proportion of primitive hematopoietic subsets and improves the number of long-term colony-forming units in CD34+ umbilical cord blood cell experiments^[2].
Stemregenin 1 (GMP) (3, 6, 8, 10 μM; 4-7 days) inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage experiments, reduces the expression of genes such as NFATc1 and ACP5, and F-actin ring formation^[3].
In Vivo:Stemregenin 1 (GMP) (2.5 mg/kg; intraperitoneal injection; once every 3 days; 42 days) reverses bone loss, reduced osteoclast numbers and increased bone mineral density in the ovariectomized (OVX) mouse osteoporosis model^[3].