Bioactivity | B7/CD28 interaction inhibitor 1 (copmound 6b) is a potent B7.1-CD28 interaction inhibitor with an IC50 of 50 nM[1]. | ||||||||||||
Target | IC50: 50 nM (B7.1-CD28 interaction) | ||||||||||||
Invitro | Bivalent CTLA4 homodimers bridge bivalent B7.1 homodimers to form an unusually stable signaling complex. Blocking B7/CD28 interactions with monoclonal antibodies or soluble receptors results in immunosuppression and enhanced allograft survival, while B7/CTLA-4 blockade results in enhanced antitumor immune responses. The interaction of co-stimulatory molecules on T cells with B7 molecules on antigen presenting cells plays an important role in the activation of naive T cells. Consequently, agents that disrupt these interactions should have applications in treatment of transplant rejection as well as autoimmune diseases[1]. | ||||||||||||
Name | B7/CD28 interaction inhibitor 1 | ||||||||||||
CAS | 635324-72-0 | ||||||||||||
Formula | C21H13F4N5O | ||||||||||||
Molar Mass | 427.35 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Green NJ, et al. Structure-activity studies of a series of dipyrazolo[3,4-b:3',4'-d]pyridin-3-ones binding to the immune regulatory protein B7.1. Bioorg Med Chem. 2003 Jul 3;11(13):2991-3013. |