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BSP16

  Cat. No.:  DC72041   Featured
Chemical Structure
2727249-47-8
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More than 5000 active chemicals with high quality for research!
Field of application
BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2727249-47-8
Chemical Name: BSP16
SMILES: COC1=C(OC)C=C([Se]C(C(C[C@@H](CC)C(O)=O)=O)=C2)C2=C1
Formula: C16H18O5Se
M.Wt: 369.27
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.
Target: IC50 for STING: 9.24 μM (ISG-THP1 cells); 5.71 μM (ISGRAW264.7 cells)[1]
In Vivo: BSP16 (po, 50 mg/kg; iv, 5 mg/kg) has well lerated and excellent pharmacokinetic profile[1]. BSP16 (oral, 15 and 30 mg/kg, q3d; oral, 20 mg/kg, q5d) induces tumor regression and durable antitumor immunity[1]. Animal Model: MC38 (colon carcinoma) syngeneic tumor model[1] Dosage: 15, 30 mg/kg Administration: oral, q3d Result: Exhibited tolerated and excellent antitumor efficacy, experienced complete tumor regression (CR) after day 21. Resulted in robust induction of IFNB and IL6 (30 mg/kg). Animal Model: CT26 (colon carcinoma) tumor model[1] Dosage: 20 mg/kg Administration: oral, q5d Result: Exhibited tolerated and induced tumor regression in all treated mice within 30 days. Led to a substantial elevation of IFNB in the plasma in CT26 bearing mice. Animal Model: Rats[1] Dosage: 5 mg/kg, 50 mg/kg Administration: oral and i.v Result: compd. adm. Cmax(μg/mL) AUG0-∞(h*μg/mL) t1/2(h) Vss(L/kg) CL(L/h/kg) F(%) BSP16 po(50 mg/kg) 58.2 315.9 1.60 0.38 0.16 107 iv(5 mg/kg) 29.4 1.04 0.26 0.17
In Vitro: BSP16 (0.1-100 μM) can selectively stimulate the STING pathway in ISG-THP1 and ISGRAW264.7 cells with EC50 values of 9.24 and 5.71 μM, respectively[1]. BSP16 (10, 25, 50 μM; 1, 3, 6 h) strongly activates STING signaling in human and mouse cells and binds STING as a homodimer[1]. BSP16 exhibits a promising absorption, distribution, metabolism, excretion and toxicity[1]. RT-PCR[1] Cell Line: ISG-THP1 cells Concentration: 10, 25, 50 μM Incubation Time: 1, 3, 6 h Result: Robustly induced mRNA expression of target genes IFNβ, CXCL10, and IL6 in response to STING activation, in a time and concentration-dependent manner in ISGTHP1 cells. Western Blot Analysis[1] Cell Line: ISG-THP1 cells Concentration: 10, 25, 50 μM Incubation Time: 1, 3, 6 h Result: Rapidly increased the phosphorylation of TBK1 and IRF3 in a concentration-dependent manner.
References: [1]. Xi Feng, et al. Discovery of Selenium-Containing STING Agonists as Orally Available Antitumor Agents. J Med Chem. 2022 Sep 7.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC60500 NVS-STG2 NVS-STG2 is a small molecule STING agonist with AC50 of 5.2 μM. NVS-STG2 induces the high-order oligomerization of human STING by binding to a pocket between the transmembrane domains of the neighboring STING dimers and elicit potent STING-mediated immune responses in cells and antitumor activities in animal models.
DC60034 STING inhibitor-1 STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-​mediated disease.
DC60033 STING INHIBITOR-2 STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING-​mediated disease.
DC39220 STING agonist compound 17 STING agonist compound 17 is a selective stimulator of interferon genes (STING) receptor agonist.
DC39210 MSA-2 analogue MSA-2 analogue is an orally available human STING agonist.
DC39031 MSA-2 MSA-2 is an orally available human STING agonist.MSA-2 is bound to STING as a noncovalent dimer. Extensive experimental analysis indicates that MSA-2 predimerization is required for binding. Acidic tumor microenvironments favor permeable, uncharged MSA-2.
DC39030 SR-717 SR-717 is a non-nucleotide, small-molecule STING agonist and functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same "closed" conformation of STING.SR-717 functions as a direct cyclic guanosine mo
DC72041 BSP16 BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.
DC50039 3'3'-cGAMP (sodium salt) 3’3’-cGAMP Fluorinated (c-[2'FdGMP]-[2'FdAMP]) is a synthetic analog of cyclic guanosine monophosphate- adenosine monophosphate (cyclic GMP-AMP, cGAMP) with a fluorine atom at 2’ position of the nucleosides. 3’3’-cGAMP is a cyclic di-nucleotide produced by bacteria. It is also referred to as "canonical" cGAMP due the presence of the classical 3’-5’ phosphodiester linkages between the guanosine and the adenosine. It has been reported that cGAMP binds STING (stimulator of IFN genes) and subsequently induces TBK1-IRF3-dependent production of IFN-β [1]. The incorporation of fluorine into biologically active molecules is commonly used in medicinal chemistry to improve their metabolic stability or to modulate physicochemical properties such as lipophilicity [2, 3]. Moreover, the introduction of a fluorine atom can change the biological activities of a molecule. Interestingly, when used at low concentrations in various cellular assays, 3’3’-cGAMP Fluorinated induces higher levels of type I IFNs than does cGAMP. STING ligands such as cGAMP induce type I IFNs and activate interferon stimulated genes (ISG) through IRFs. To facilitate their study, InvivoGen has developed stable reporter cells in two well established immune cell models: THP-1 human monocytes and RAW 264.7 murine macrophages. These cells express a reporter gene (SEAP or Lucia luciferase), under control of an IRF-inducible promoter.
DC48024 cGAMP diammonium cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
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