Stemregenin 1  (Synonyms: SR1)

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: 127 nM (AhR)^[4]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

429.54

C₂₄H₂₃N₅OS

1227633-49-9

Solid

Off-white to yellow

CC(C)N1C2=NC(C3=CSC4=C3C=CC=C4)=NC(NCCC5=CC=C(O)C=C5)=C2N=C1

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

• [1]. Tao L, et al. StemRegenin 1 selectively promotes expansion of Multipotent Hematopoietic Progenitors derived from Human Embryonic Stem Cells. J Stem Cells Regen Med. 2017 Dec 18;13(2):75-79.  [Content Brief]

  [2]. Jackson CS, et al. Targeting the aryl hydrocarbon receptor nuclear translocator complex with DMOG and Stemregenin 1 improves primitive hematopoietic stem cell expansion. Stem Cell Res. 2017 May;21:124-131.  [Content Brief]

  [3]. Zhou S, et al. StemRegenin 1 attenuates the RANKL-induced osteoclastogenesis via inhibiting AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway. iScience. 2024 Apr 6;27(5):109682.  [Content Brief]

  [4]. Boitano AE, et al. Aryl Hydrocarbon Receptor Antagonists Promote the Expansion of Human Hematopoietic Stem Cells. Science. 2010 Sep 10;329(5997):1345-8.  [Content Brief]