In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BIIB021 is a selective inhibitor of Hsp90 with Ki and EC50 values of 1.7 nM and 38 nM, respectively.
HSP90 (heat shock protein 90) is widely expressed as a molecular chaperone. It plays a major role in the folding and stabilization of cellular proteins. HSP90 protects client proteins from degradation and maintains them in an active conformation. Many clients of HSP90 are transcription factors or protein kinases such as: Bcr-Abl, tyrosine kinases, EGFR family members, IGF1-R, c-Met, steroid hormone receptors, p53, Mdm2 and telomerase. In a variety of cancers, overexpressed hsp90 has been found. Hsp90 also play an important role in maintaining the transformed phenotype of cancer cells so. Hsp 90 is one attractive target for cancer therapy.
BIIB021 competitive binds in the ATP-binding pocket and inhibits Hsp90 chaperone function, and lead to client protein degradation, cell death and tumor growth inhibition. BIIB021 leads to degradation of HER-2 which is an Hsp90 client protein. BIIB021 can also the growth of a variety of cancer cell lines in cell proliferation assays. In MCF-7 cells, BIIB021 leaded to HER-2 degradation with the EC50 value of was38 ± 10 nmol/L. BIIB021 inhibit the cell proliferation with IC50 values of 0.06 μ mol/L in N87 cells, 0.31μ mol/L in MCF-7 cells and 0.14 μ mol/L in BT474 cells. In MCF-7 cells, BIIB021 significantly reduced the phosphorylation levels of HER-2 at a concentration of 50 nM. BIIB021 selectively inhibited Hodgkin's lymphoma cell viability at nanomolar concentrations but not in lymphocytes from healthy individuals. BIIB021 can increase the susceptibility to NK cell mediated killing by inducing the expression of ligands for the activating NK cell receptor NKG2D on Hodgkin's lymphoma cells. BIIB021 reduced the expression of key radioresponsive proteins, then enhanced the radiosensitivity of HNSCCA cell lines in vitro, increased apoptosis cells and induced G2 arrest.
BIIB021 showed significant activity at doses of 31,62.5, and 125 mg/kg in human in nude mice bearing N87 stomach carcinoma tumors. HSP90 significantly inhibited tumor growth in a xenograft model of Hodgkin's lymphoma.
1.Lundgren K, Zhang H, Brekken J, Huser N, Powell RE, Timple N, Busch DJ, Neely L, Sensintaffar JL, Yang YC et al: BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol Cancer Ther 2009, 8(4):921-929.
2.Yin X, Zhang H, Lundgren K, Wilson L, Burrows F, Shores CG: BIIB021, a novel Hsp90 inhibitor, sensitizes head and neck squamous cell carcinoma to radiotherapy. Int J Cancer 2010, 126(5):1216-1225.
3.Boll B, Eltaib F, Reiners KS, von Tresckow B, Tawadros S, Simhadri VR, Burrows FJ, Lundgren K, Hansen HP, Engert A et al: Heat shock protein 90 inhibitor BIIB021 (CNF2024) depletes NF-kappaB and sensitizes Hodgkin's lymphoma cells for natural killer cell-mediated cytotoxicity. Clin Cancer Res 2009, 15(16):5108-5116.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥14.95 mg/mL in DMSO,insoluble in EtOH，insoluble in H2O|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|
|Description||BIIB021 is a selective and competitive inhibitor of Hsp90 with Ki value of 1.7 nM.|
|IC50||1.7 nM (Ki)|