WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406523
CAS#: 1334493-07-0
Description: BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor. BP-1-102 binds Stat3 with an affinity (K(D)) of 504 nM, blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8, which is identified as a Stat3 target gene that promotes Stat3-mediated breast tumor cell migration and invasion.
Hodoodo Cat#: H406523
Name: BP-1-102
CAS#: 1334493-07-0
Chemical Formula: C29H27F5N2O6S
Exact Mass: 626.15
Molecular Weight: 626.590
Elemental Analysis: C, 55.59; H, 4.34; F, 15.16; N, 4.47; O, 15.32; S, 5.12
Synonym: BP-1-102; BP1-102; BP 1-102; BP1102; BP-1102; BP 1102.
IUPAC/Chemical Name: 4-(N-(4-cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)-2-hydroxybenzoic acid
InChi Key: WNVSFFVDMUSXSX-UHFFFAOYSA-N
InChi Code: InChI=1S/C29H27F5N2O6S/c1-35(43(41,42)28-26(33)24(31)23(30)25(32)27(28)34)15-22(38)36(19-11-12-20(29(39)40)21(37)13-19)14-16-7-9-18(10-8-16)17-5-3-2-4-6-17/h7-13,17,37H,2-6,14-15H2,1H3,(H,39,40)
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
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | BP-1-102 is an inhibitor of transcription factor Stat3 with an IC50 of 6.8 μM. |
In vitro activity: | AGS and HGC-27 cells were exposed to various concentrations of BP-1-102 to evaluate its effect on the proliferation of GC (gastric cancer) cells using a CCK8 assay. Compared with the control group, BP-1-102 treatment dose-dependently suppressed the proliferation of AGS cells (Fig. 2A) but had no such inhibitory effect on HGC-27 cells (Fig. 2B). Furthermore, the results of the colony formation assays showed that the BP-1-102-treated AGS cells formed smaller and fewer colonies compared with those in the control group. BP-1-102 was less effective towards HGC-27 cells than AGS cells (Fig. 2C and D). These results indicated that BP-1-102 exerted a tumor suppressive role in GC cells lines and that this effect was enhanced by high expression levels of p-STAT3 (Y705). Reference: Mol Med Rep. 2019 Apr;19(4):2698-2706. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6423579/ |
In vivo activity: | The role of BP-1-102, an oral bioavailable STAT3 inhibitor, in IA (intracranial aneurysms) was investigated. An IA mouse model was constructed by injecting elastase into the cerebrospinal fluid with simultaneous induction of hypertension by deoxycorticosterone acetate (DOCA) implantation. The results showed that the proportion of IA rupture in mice after BP-1-102 administration was significantly reduced, and the survival time was significantly extended. Further research showed that compared with the Vehicle group, the proportion of macrophages infiltrated at the aneurysm and the expression of pro-inflammatory cytokines in the BP-1-102 administration group were significantly reduced. Reference: J Drug Target. 2021 Mar 8:1-25. https://www.tandfonline.com/doi/abs/10.1080/1061186X.2021.1895817?journalCode=idrt20 |
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 15.0 | 23.90 |
The following data is based on the product molecular weight 626.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | 1. Jiang X, Tang J, Wu M, Chen S, Xu Z, Wang H, Wang H, Yu X, Li Z, Teng L. BP‑1‑102 exerts an antitumor effect on the AGS human gastric cancer cell line through modulating the STAT3 and MAPK signaling pathways. Mol Med Rep. 2019 Apr;19(4):2698-2706. doi: 10.3892/mmr.2019.9892. Epub 2019 Jan 24. PMID: 30720080; PMCID: PMC6423579. 2. Wu QY, Cheng Z, Zhou YZ, Zhao Y, Li JM, Zhou XM, Peng HL, Zhang GS, Liao XB, Fu XM. A novel STAT3 inhibitor attenuates angiotensin II-induced abdominal aortic aneurysm progression in mice through modulating vascular inflammation and autophagy. Cell Death Dis. 2020 Feb 18;11(2):131. doi: 10.1038/s41419-020-2326-2. PMID: 32071300; PMCID: PMC7028955. 3. Jiang Z, Huang J, You L, Zhang J. BP-1-102, a STAT3 inhibitor, reduces intracranial aneurysm rupture and suppresses inflammatory responses in a mouse model. J Drug Target. 2021 Mar 8:1-25. doi: 10.1080/1061186X.2021.1895817. Epub ahead of print. PMID: 33682559. |
In vitro protocol: | 1. Jiang X, Tang J, Wu M, Chen S, Xu Z, Wang H, Wang H, Yu X, Li Z, Teng L. BP‑1‑102 exerts an antitumor effect on the AGS human gastric cancer cell line through modulating the STAT3 and MAPK signaling pathways. Mol Med Rep. 2019 Apr;19(4):2698-2706. doi: 10.3892/mmr.2019.9892. Epub 2019 Jan 24. PMID: 30720080; PMCID: PMC6423579. 2. Wu QY, Cheng Z, Zhou YZ, Zhao Y, Li JM, Zhou XM, Peng HL, Zhang GS, Liao XB, Fu XM. A novel STAT3 inhibitor attenuates angiotensin II-induced abdominal aortic aneurysm progression in mice through modulating vascular inflammation and autophagy. Cell Death Dis. 2020 Feb 18;11(2):131. doi: 10.1038/s41419-020-2326-2. PMID: 32071300; PMCID: PMC7028955. |
In vivo protocol: | 1. Jiang Z, Huang J, You L, Zhang J. BP-1-102, a STAT3 inhibitor, reduces intracranial aneurysm rupture and suppresses inflammatory responses in a mouse model. J Drug Target. 2021 Mar 8:1-25. doi: 10.1080/1061186X.2021.1895817. Epub ahead of print. PMID: 33682559. 2. Wu QY, Cheng Z, Zhou YZ, Zhao Y, Li JM, Zhou XM, Peng HL, Zhang GS, Liao XB, Fu XM. A novel STAT3 inhibitor attenuates angiotensin II-induced abdominal aortic aneurysm progression in mice through modulating vascular inflammation and autophagy. Cell Death Dis. 2020 Feb 18;11(2):131. doi: 10.1038/s41419-020-2326-2. PMID: 32071300; PMCID: PMC7028955. |
1: Zhang X, Yue P, Page BD, Li T, Zhao W, Namanja AT, Paladino D, Zhao J, Chen Y, Gunning PT, Turkson J. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9623-8. doi: 10.1073/pnas.1121606109. Epub 2012 May 23. PubMed PMID: 22623533; PubMed Central PMCID: PMC3386073.