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MEISi-2 is a specific MEISi inhibitor that inhibits the meis luciferase reporter gene in vitro and induces MEIS-dependent hematopoietic stem cell maintenance and self-renewal, which can be used in research areas such as cardiac injury, hematopoietic problems, bone marrow transplantation and cancer.

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with an IC50 of 574 nM. It acts independently of Ca 2+ and inhibits Nigericin-induced inflammasome activation in THP-1 cells, as well as Imiquimod-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

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.

Imupedone (LF 1695) is a synthetic immunomodulator that modulates T lymphocytes and macrophages, induces T-cell differentiation of bone marrow precursor cells, and increases the proliferative response of lymphocytes to mitogens, antigens, and allogeneic cells.13483-84-5

Batilol (Stearyl monoglyceride), isolated from shark liver oil, is also present in yellow bone marrow of animals and has been described as an inflammatory agent.

Mitotane (NCI-C04933) is a derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

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.

Hydroxysafflor yellow A (Safflomin A) inhibits adipogenesis by increasing HSL promoter activities, effectively protects the liver from long-term alcohol injury by enhancing antioxidant capacity and inhibiting the expression of TGF-β, prevents steroid-induced avascular necrosis of the femoral head by inhibiting primary bone marrow-derived mesenchymal stromal cells, and exhibits anti-tumor effects.

Entospletinib (GS-9973) (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable.

UUN44923 is a FTO inhibitor. It may be useful for treating diseases assocd. with FTO targets, obesity, metabolic syndrome (MS) , type 2 diabetes (T2D) , Alzheimer's diseases, breast cancers, small- cell lung cancers, a human bone marrow striated muscle cancer, a pancreatic cancer, malignant glioblastoma and the like.

NDMC101 is an inhibitor of dipeptidyl peptidase-IV activity in human T cells and exhibits immunomodulatory effects. It also acts as a novel inhibitor of NFATc1 and NF-κB activity.

MNITMT is a potent immunosuppressive agent without bone marrow toxicity [1].

Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).

Acetyl Ser-Asp-Lys-Pro is formed in bone marrow cells by enzymatic processing of thymosin β4. It inhibits the entry of pluripotent hemopoietic stem cells into S-phase of the cell cycle and protects against Ara-C lethality in mice.

KLD-12, a 12-residue self-assembling peptide, displays properties that promote chondrogenic differentiation of bone marrow stromal cells (BMSCs). Moreover, KLD-12 hydrogel can effectively fill full-thickness osteochondral defects in their original location, leading to improved cartilage repair.

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.

4α-Phorbol is a derivative of PKC activator 12 myristate 13 acetate. Can induce chromosomal damage in ex vivo mouse bone marrow red blood cells.

CXM102 is an activator of autophagy. This compound induces autophagy in aged BMSCs, rejuvenating them and promoting their preferential differentiation into osteoblasts. CXM102 enhances the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. In middle-aged male mice, it stimulates bone anabolic metabolism, reduces marrow adipocytes, delays bone loss, lowers serum inflammation levels, reduces organ fibrosis, and extends lifespan.

NLRP3-IN-49 (compound Z48) is a potent and specific inhibitor of NLRP3, displaying IC50 values of 0.26 μM in THP-1 cells and 0.21 μM in mouse bone marrow-derived macrophages. It directly binds to the NLRP3 protein with a dissociation constant (Kd) of 1.05 μM, effectively preventing the assembly and activation of the NLRP3 inflammasome, thereby exhibiting anti-inflammatory properties. NLRP3-IN-49 is utilized in the research of inflammatory bowel disease.

FR 900490 is an immunoactive substance produced by a fungus Discosia sp. F-11809. In vitro FR-900490 restores the colony forming units in culture (cfu-c) in bone marrow cells, which were suppressed by immunosuppressive factor obtained from the serum of sa

AZD2906, a selective glucocorticoid receptor (GR) agonist, demonstrates inhibitory concentrations (IC50s) of 2.2 nM in human GR, 0.3 nM in rat peripheral blood mononuclear cells (PBMC), 41.6 nM in human whole blood, and 7.5 nM in rat whole blood, respectively[1]. Additionally, it induces an increase in micronucleated immature erythrocytes within rat bone marrow.

1-Hydroxy-2,3,5-trimethoxyxanthone (HM-1) exhibits vasodilator action through an endothelium-dependent mechanism involving NO and an endothelium-independent mechanism by inhibiting Ca(2+) influx via L-type voltage-operated Ca(2+) channels. A minor contribution to HM-1's effects may stem from inhibiting protein kinase C-mediated release of intracellular Ca(2+) stores. At 1 µg mL, HM-1 effectively inhibits osteoclast differentiation in co-cultures with mouse osteoblastic calvarial and bone marrow cells and protects mice from acute lung injury induced by lipopolysaccharide (LPS), likely by increasing IκB-α protein expression and suppressing inducible nitric oxide synthase and cyclooxygenase-Ⅱ protein expression.