stromal

Etonogestrel (Implanon) is a steroidal progestin used as hormonal contraceptives.

Tigogenin is one of steroidal sapogenins which is widely used for synthesizing steroid drugs. It might have protective effect on bone and be helpful in preventing the development of osteoporosis.

N-Oleoyl-L-Serine (N-Oleoylserine) is an endogenous long-chain fatty acid amide that is a lipid modulator of bone remodeling and stimulates osteoclast apoptosis which can be used to study osteoporosis. N-Oleoyl-L-Serine showed high activity in an osteoblast proliferation assay.N-Oleoyl-L-Serine promotes osteoclast apoptosis by inhibiting Erk1/2 phosphorylation and expression of nuclear κB ligand (RANKL) receptor activator in bone marrow stromal cells and osteoblasts, which attenuates osteoclast populations.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

Plerixafor octahydrochloride (JM3100 octahydrochloride) blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity.

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

c-Kit-IN-2 is a c-KIT-targeted inhibitor with an IC₅₀ of 82 nM. It exhibits favorable anti-proliferative effects on three gastrointestinal stromal tumor cell lines GIST882, GIST430, and GIST48, with corresponding GI₅₀ values of 3 nM, 1 nM, and 2 nM, respectively.

ML-9 (free base) suppresses MLCK, PKA, and PKC activity (Ki: 4, 32, and 54 μM, respectively). ML-9 (free base) is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) acti

ML-9 suppresses MLCK, PKA, and PKC activity with Ki values of 4, 32, and 54 μM, respectively. ML-9 is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) activity. ML-9 causes autophagy by stimulating autophagosome formation and inhibiting their degradation.

Pyr10 is a pyrazole derivative and a selective TRP cation 3 inhibitor that distinguishes between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells (IC50: 0.72 μM) and has an IC50 of 13.08 μM for store-operated Ca2+ entry in BRL-2H3 cells.

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. USL311 inhibits CXCR4 activation and decreases proliferation and migration of CXCR4-expressing tumor cells, with anti-tumor activ

Burixafor (also known as TG-0054) is an orally available inhibitor of the CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell mobilization activities. By binding to the CXCR4 chemokine receptor, Burixafor blocks the binding and subsequent activation of stromal cell-derived factor-1 (SDF-1 or CXCL12) with the CXCR4 receptor, potentially facilitating the mobilization of hematopoietic stem and progenitor cells from the bone marrow into the bloodstream. Note: Elemental analysis shows that this compound is a salt containing 3 HBr and 3 water molecules.

KIT/PDGFRA-IN-1 (compound 19) is an inhibitor targeting the stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA). Its IC50 values are 2.3 µM for KIT-wt, 12 µM for KIT-D816H, 492 µM for KIT-T670I, 0.8 µM for PDGFRA-wt, 99.9 µM for PDGFRA-D842V, 42.3 µM for PDGFRA-T674I, and 4.3 µM for PDGFRA-G680R. The GR50 values for GIST-T1, T1-a-D842V, and GIST-48B cell lines (gastrointestinal stromal tumor cell lines with PDGFR and KIT mutations) are 12 nM, 8900 nM, and ≥10,000 nM, respectively.

PDGFRαkinase inhibitor 3 (Compound L7) is a potent inhibitor targeting the PDGFRαD842V kinase, exhibiting IC50 values of 23.8 nM in biochemical assays and 2.1 nM in cellular assays. It binds to the ATP binding site of PDGFRαD842V, blocking downstream signaling pathways and inhibiting kinase activity. PDGFRαkinase inhibitor 3 is applicable in gastrointestinal stromal tumor (GIST) research.

KN-17, a modified derivative based on the cecropin B structure, effectively disrupts bacterial growth and induces the migration of human bone marrow stromal cells (hBMSCs). This compound significantly stimulates angiogenesis both in vitro and in vivo.

TOP5300 is an orally active allosteric agonist of the follicle-stimulating hormone receptor (FSHR). It induces testosterone production in stromal cells and promotes folliculogenesis and superovulation in rats.

TOP5668 is an orally active allosteric agonist of the follicle-stimulating hormone receptor. It induces testosterone production in stromal cells and enhances folliculogenesis and superovulation in rats.

Raloxifene alkene (Compound 101) is a significant serum cholesterol-clearing agent. It exhibits notable antiproliferative activity against breast cancer cells. In an ovariectomized rat model, Raloxifene alkene effectively reduces serum cholesterol levels without significantly increasing uterine weight or the number of eosinophils in stromal cells. This compound is applicable for research into postmenopausal syndrome, particularly osteoporosis, estrogen-dependent breast cancer, and uterine cancer.

c-KitReceptor modulator-1 (Compound #22) is a regulator of the c-Kit receptor. This compound is applicable in research focused on malignant cancers such as canine mast cell tumors, human gastrointestinal stromal tumors, and small cell lung cancer.

TH301 acts as a stabilizer for cryptochrome circadian regulator 2 (CRY2). It demonstrates selectivity by stabilizing CRY2 over CRY1 in a degradation assay conducted with HEK293 cells expressing CRY reporters at concentrations ranging from 0.1 to 10 µM. In wild-type mouse fibroblasts, TH301 extends the circadian period, but this effect is absent in Cry2-/- fibroblasts. Additionally, it boosts rosiglitazone-dependent induction of brown adipose tissue-specific genes such as Ucp1, Cidea, and Kcnk3 in primary mouse stromal vascular fractions.

4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE is a component of a drug-linker conjugate for ADC. It includes a linker and a biologically active small molecule toxin, MMAE. This compound can conjugate with NN2101 (anti-c-Kit) to form NN3201, which rapidly internalizes and inhibits SCF-driven signal transduction, inducing cell cycle arrest and apoptosis through payload delivery. NN3201 exhibits significant c-Kit-dependent antitumor activity in various tumor models, such as small cell lung cancer (SCLC) and gastrointestinal stromal tumors (GIST).

Imatinib is a multi-target inhibitor of v-Abl, c-Kit, and PDGFR (IC50: 0.6 μM, 0.1 μM, and 0.1 μM, respectively). Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs), and a number of other malignancies.

Glycitin (Glycitein 7-O-β-glucoside), a natural isoflavone isolated from legumes, promotes the proliferation of bone marrow stromal cells and osteoblasts while suppressing bone turnover.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.