Buforin IIb TFA
Buforin IIb TFA (BF2-B TFA) is an anticancer peptide, as well as an Antibacterial and Antifungal agent. Buforin IIb TFA is derived from histone H2A. Buforin IIb TFA activates SAPK/JNK and p38 MAPK. Buforin IIb TFA induces mitochondria-dependent Apoptosis. Buforin IIb TFA achieves selective targeting by interacting with gangliosides on the surface of cancer cells, and can penetrate cancer cell membranes without causing damage. Buforin IIb TFA exhibits antibacterial activity against Gram-negative bacteria, Gram-positive bacteria and fungi. Buforin IIb TFA can be used in the research of cervical cancer, as well as cancers including leukemia, central nervous system cancer, ovarian cancer, breast cancer, melanoma, colon cancer, non-small cell lung cancer, renal cancer and prostate cancer.
For research use only. We do not sell to patients.
- Formula: C115H207N43O23·xC2HF3O2
- Molecular Weight:2560.15 (free base)
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Buforin IIb (4 μM; 3-24 h) TFA induces time-dependent activation of SAPK/JNK and p38 MAPK in HeLa cells, which is downstream of ER stress and Ca2+ release from the ER[1].
Buforin IIb (4 μM; 3-24 h) TFA induces time-dependent dysregulation of Bcl-2 family proteins, mitochondrial translocation of Bax, and cytochrome c release in HeLa cells, which are downstream of ER stress and MAPK activation[1].
Buforin IIb (0-200 μg/mL; 48 h) TFA potently and selectively kills cancer cells, with IC50 values of 6 μg/mL for Jurkat cells, 12 μg/mL for HeLa cells, 7.2-23.9 μg/mL for 60 diverse human tumor cell lines, and ~350 μg/mL for normal human fibroblasts, mouse embryonic fibroblasts, and peripheral blood lymphocytes[2].
Buforin IIb (20 μg/mL; 24 h) TFA induces mitochondria-dependent apoptosis in Jurkat and HeLa cancer cells, as shown by annexin V/PI staining, DNA fragmentation, and activation of caspase-9, caspase-3, and PARP cleavage[2].
Buforin IIb (24 h) TFA inhibits growth of Escherichia coli K12D31 (MIC 0.4 μM), Bacillus subtilis CGMCC 1.1087, and Saccharomyces cerevisiae CGMCC 2.399 (MIC 1.5 μM) with activity comparable to synthetic buforin IIb[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human cervical adenocarcinoma HeLa cells
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Concentration:4 μM
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Incubation Time:3 h, 6 h, 12 h, 24 h
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Result:Caused a time-dependent increase in protein levels of phosphorylated protein kinase-like endoplasmic reticulum kinase (p-PERK, Thr980), phosphorylated inositol-requiring protein 1 (p-IRE1, Ser724), 78 kDa glucose-regulated protein (GRP78), and C/EBP homologous protein (CHOP), a hallmark of ER stress-mediated apoptosis.\nActivated stress-activated protein kinase/Jun-amino-terminal kinase (SAPK/JNK) and p38 mitogen-activated protein kinase (MAPK), with increased phosphorylation detected from 6 h onward.
Blocked activation of both kinases when cells were pretreated with specific MAPK inhibitors (SP600125 for SAPK/JNK, SB203580 for p38 MAPK), as well as by pretreatment with ER stress inhibitor PBA or Ca2+ chelator BAPTA/AM.\nCaused time-dependent downregulation of anti-apoptotic Bcl-xL and Bcl-2.
Increased translocation of pro-apoptotic Bax from the cytosol to mitochondria.
Induced time-dependent release of cytochrome c from mitochondria to the cytosol.
Abolished these effects when cells were pretreated with SAPK/JNK inhibitor SP600125, p38 MAPK inhibitor SB203580, or ER stress inhibitor PBA.
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Cell Line:Jurkat human leukemia cells, HeLa human cervical cancer cells, human fibroblasts, mouse embryonic fibroblasts, peripheral blood lymphocytes, 60 diverse human tumor cell lines (leukemia, CNS cancer, ovarian cancer, breast cancer, melanoma, colon cancer, non-small cell lung cancer, renal cancer, prostate cancer)
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Concentration:0-200 μg/mL
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Incubation Time:48 h
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Result:Exhibited selective cytotoxicity with IC50 values of 6 μg/mL for Jurkat cells, 12 μg/mL for HeLa cells.
Showed potent cytotoxicity against 60 human tumor cell lines with IC50 values ranging from 7.2 μg/mL (HOP-92 non-small cell lung cancer) to 23.9 μg/mL (T-47D breast cancer).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (nu/nu)[2]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.v.; days 1, 2, 4, 8
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Result:Suppressed tumor growth compared to PBS controls.
Reduced mean tumor volume substantially relative to control group (~1000 mm3) by study completion (day 20).
Induced statistically significant difference (P < 0.05) in tumor volume compared to controls starting on day 8 through study end.
Chemical Information
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Molecular Weight 2560.15 (free base)
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Formula C115H207N43O23·xC2HF3O2
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SMILES
O=C(N[C@@H](C)C(NCC(N[C@@H](CC(C)C)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC1=CC=CC=C1)C(N2[C@@H](CCC2)C(N[C@@H](C(C)C)C(NCC(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCCNC(N)=N)N.OC(C(F)(F)F)=O.[x]
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Synonyms
BF2-B TFA
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Sequence
Arg-Ala-Gly-Leu-Gln-Phe-Pro-Val-Gly-Arg-Leu-Leu-Arg-Arg-Leu-Leu-Arg-Arg-Leu-Leu-Arg
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Sequence Shortening
RAGLQFPVGRLLRRLLRRLLR
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[2]. Lee HS, et al. Mechanism of anticancer activity of buforin IIb, a histone H2A-derived peptide. Cancer letters. 2008 Nov 18;271(1):47-55. [Content Brief]
[3]. Wang Q, et al. Expression and purification of antimicrobial peptide buforin IIb in Escherichia coli. Biotechnology letters. 2011 Nov;33(11):2121-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Buforin IIb TFA Related Classifications
HY-P12127A Related Classifications
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