bmp-2

BMP agonist 2 has up-regulated bone morphogenetic protein BMP-2 expression activity in vivo and anti-osteoporosis effects, and also has ameliorated the symptoms of osteoporosis in SAMP6 mice.BMP agonist 2 is an osteoinductive cytokine that promotes the production of bone tissue, and can be used in the study of senile osteoporosis (SOP).

BMT-124110 Formate is a selective AAK1 inhibitor (IC50: 0.9 nM) with anti-injury sensory activity.BMT-124110 Formate inhibits the BMP-2-inducible protein kinase BIKE with an IC50: 17 nM.BMT-124110 Formate inhibits the cell-cycle protein G-related BMT-124110 Formate inhibits the cell cycle protein G-associated kinase GAK with an IC50:99 nM.

BMT-124110 is a selective AAK1 inhibitor (IC50: 0.9 nM) with antinociceptive activity. BMT-090605 inhibited BMP-2 induced protein kinase BIKE with IC50 of 17 nM. BMT-090605 inhibits cyclin G-associated kinase GAK with an IC50 of 99 nM.

LP-922761 is a potent, selective, and orally active AAK1 inhibitor with inhibitory effects on BMP-2 induced protein kinase (BIKE).

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8/0.8/5.3/16.7 nM for ALK1/2/3/6).

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.

BMP Agonist 1 (compound 2 b) is a small-molecule stimulator of bone morphogenic protein (BMP) signaling, crucial for the differentiation of C2C12 cells. It acts by inhibiting GSK3β and enhancing β-catenin signaling, thereby synergistically modulating Id2 and Id3 expression. This compound is employed in skeletal disease and defect research [1].

BMP2-derived peptide, encompassing amino acids 73 to 92 of BMP-2, induces osteogenic differentiation in bone marrow stromal cells (BMSCs) and augments bone regeneration [1].

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

1. Kirenol (Kirel) has anti-oxidant, anti-inflammatory, anti-allergic, and anti-arthritic activities. 2. Kirenol is effective against gram-positive bacteria. 3. Kirenol possesses antitumor action on human chronic myeloid leukemia K562 cells in vitro. 4. Kirenol is capable of promoting osteoblast differentiation in MC3T3-E1 cells through activation of the BMP and Wnt/β-catenin signaling pathways. 5. Kirenol treatment reduces pro-inflammatory cytokine secretion, increases anti-inflammatory cytokine production, inhibits cell proliferation and induces apoptosis of CII-specific lymphocytes in vitro.

ER 50891 quarterhydrate is a potent RARα (retinoic acid receptor α) antagonist that markedly diminishes the inhibitory effects of ATRA (all-trans retinoic acid) on osteoblastogenesis induced by BMP 2 (bone morphogenetic protein 2) [1].

Asperosaponin VI (Akebia saponin D) , the most abundant constituent of the rhizome of Dipsacus asper, has been used for the treatment of lower back pain, traumatic hematoma and bone fractures.

Mevastatin (ML236B) is an HMG-CoA reductase inhibitor that was initially isolated from the mold Pythium ultimum. Mevastatin was the first statin to enter clinical trials.

LP-922761 hydrate is a selective, potent, orally active AAK1 inhibitor with IC50 values of 4.8 nM and 7.6 nM in enzyme and cellular assays, respectively. LP-922761 hydrate inhibits BMP-2 inducible protein kinase (BIKE) (IC50: 24 nM). 922761 hydrate has no significant effect on cellular GAK, opioids, adrenergic α2 or GABAa receptors.

K 02288 is a novel small molecule inhibitor of ALK1/2/3/6.

L-quebrachitol is a natural product.L-quebrachitol may promote osteoblastogenesis by triggering the BMP-2-response as well as the Runx2, MAPK, and Wnt β-catenin signaling pathway.

Smurf1-IN-A01 (A01) is a ubiquitin ligase Smad ubiquitination regulatory factor-1 inhibitor (kd: 3.664 nM). It increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.

BMT-090605 hydrochloride is an effective and selective inhibitor of connexin-2 associated kinase 1 (AAK1) (IC50=0.6 nM). BMT-090605 hydrochloride inhibits BMP-2 induced protein kinase (BIKE) (IC50=45 nM) and cyclin G-related kinase GAK (IC50=60 nM). BMT-090605 hydrochloride shows anti-injury activity. BMT-090605 hydrochloride has research value in neuropathic pain.

BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively[1]. BMT-090605 shows antinociceptive activity

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density volume and mineralization in vivo.