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Chemical Structure| 1334493-07-0 Chemical Structure| 1334493-07-0
Chemical Structure| 1334493-07-0

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CAS No.: 1334493-07-0

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BP-1-102 is an orally available, small-molecule inhibitor of transcription factor STAT3.

Synonyms: BP-1-102

4.5 *For Research Use Only !

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Product Details of BP-1-102

CAS No. :1334493-07-0
Formula : C29H27F5N2O6S
M.W : 626.59
SMILES Code : O=C(O)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1O
Synonyms :
BP-1-102
MDL No. :MFCD29477477
InChI Key :WNVSFFVDMUSXSX-UHFFFAOYSA-N
Pubchem ID :53388144

Safety of BP-1-102

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of BP-1-102

JAK-STAT

Isoform Comparison

Biological Activity

Target

  • STAT3

    STAT3, Kd:504 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
MDA-MB-231 4–6.8 μM 30 minutes Inhibits Stat3 activation, blocks growth, survival, migration, and invasion of Stat3-dependent tumor cells PMC3386073
NIH 3T3/v-Src 0–30 μM Suppresses cell proliferation, anchorage-dependent growth, and colony formation PMC3386073
DU145 0–20 μM 24 hours Inhibits Stat3 DNA-binding activity PMC3386073
Panc-1 0–20 μM 24 hours Inhibits Stat3 DNA-binding activity PMC3386073
A549 0–20 μM 24 hours Inhibits Stat3 DNA-binding activity PMC3386073
Human pulmonary microvascular endothelial cells (HPMECs) 5 μM 6 hours BP-1-102 inhibited LPS-induced HPMECs proliferation, enhanced endothelial integrity, reduced cytokine levels, and protected HPMECs from LPS damage through the JAK2/STAT3, NF-κB, MAPK, and AKT pathways. PMC7341624
Raw264.7 macrophages 5 μM 6 hours BP-1-102 inhibited LPS-induced macrophage proliferation, reduced cytokine and TF production, and modulated macrophage inflaμMatory response through the JAK2/STAT3, NF-κB, MAPK, and AKT pathways. PMC7341624
vascular smooth muscle cells (VSMCs) 0.05 μM, 0.1 μM, 0.5 μM 24 hours BP-1-102 inhibited AngII-induced JAK2/STAT3 and NF-κB signaling activation and maintained autophagy-related proteins expression in VSMCs. PMC7028955
DLD-1 cells 1 and 3 μg/ml 15 minutes BP-1-102 completely suppressed TIL-derived supernatant-induced STAT3 and NF-kB activation and abrogated CRC cell proliferation. PMC4493653
HT-29 cells 1 and 3 μg/ml 15 minutes BP-1-102 completely suppressed TIL-derived supernatant-induced STAT3 and NF-kB activation and abrogated CRC cell proliferation. PMC4493653
mouse oocytes 2, 4, 8, 16 μM 15 hours To investigate the effect of BP-1-102 on meiotic spindle assembly and chromosome segregation in mouse oocytes. Results showed that BP-1-102 treatment led to abnormal spindle assembly and chromosome mislocation in a dose-dependent manner. PMC7072877
Mouse bone marrow mononuclear cells 10 μM 6 days Induce differentiation of mouse bone marrow mononuclear cells into functional insulin-producing cells, expressing genes related to pancreatic beta cell development and function, such as PDX1, NKX6.1, MAFA, NEUROG3, GLUT2, and insulin. PMC10346423

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice Human breast and lung tumor xenografts Intravenous or oral gavage 20 mg/kg daily for 4 days Inhibits growth of human breast and lung tumor xenografts PMC3386073
C57BL/6 mice Cecal ligation and puncture (CLP)-induced sepsis model Intraperitoneal injection 1 or 3 mg/kg Every 2 or 3 days for 15 days BP-1-102 reduced proinflammatory factors, suppressed coagulation activation, attenuated lung injury, and improved survival rate in septic mice by inhibiting pY-STAT3 expression. PMC7341624
ApoE?/? mice AngII-induced AAA model oral 70 mg/kg Twice a week for 2 weeks BP-1-102 markedly decreased AAA incidence and aortic diameter, maintained elastin structure and volume, reduced the expression of pro-inflammatory cytokines and MMPs, and inhibited inflammatory cells infiltration. PMC7028955
mice Apcmin/+ mice oral 175 mg/kg Single injection, observed for 7 days BP-1-102 reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas. PMC4493653
Mice Streptozotocin (STZ)-induced diabetic mice Oral gavage 5 mg/kg every 2 days until day 56 Oral administration of BP-1-102, along with three other factors, induced differentiation of endogenous BMNCs into insulin-producing cells, improving blood glucose levels and insulin secretion in diabetic mice PMC11788547
Mice Focal ischemic stroke model Oral 10 mg/kg daily until sacrifice Inhibiting the STAT3 phosphorylation/activation abolished all beneficial effects of rPKM2 in the stroke mice PMC6095793
C57BL/6 mice Streptozotocin-induced diabetes model Subcapsular kidney transplantation 4 μM 7 days of culture followed by transplantation Evaluate the therapeutic effect of BP-1-102-treated bone marrow mononuclear cells in diabetic mice, showing reduced blood glucose levels, enhanced glucose tolerance, and improved insulin secretion after transplantation. PMC10346423

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.60mL

0.32mL

0.16mL

7.98mL

1.60mL

0.80mL

15.96mL

3.19mL

1.60mL
Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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