IgH Inhibitors
Chemical inhibitors of immunoglobulin heavy chain (IgH) can modulate the production and function of IgH through various molecular mechanisms. Cyclosporin A targets the calcineurin pathway by binding to cyclophilin, an intracellular protein, and forming a complex that inhibits calcineurin. This prevents the activation of transcription for interleukin-2, a cytokine pivotal in the proliferation of B-cells, subsequently affecting IgH production. Rapamycin, by forming a complex with FKBP12, inhibits the activity of mTOR Complex 1 (mTORC1), a key regulator of cell growth and proliferation. This leads to a reduction in B-cell proliferation, which in turn decreases the production and activity of IgH.
Idelalisib and Duvelisib exert their influence by selectively inhibiting the phosphoinositide 3-kinase (PI3K) pathway, with Idelalisib targeting the delta isoform and Duvelisib targeting both the gamma and delta isoforms of PI3K. This inhibition disrupts PI3K signaling, which is crucial for B-cell activation and survival, resulting in a decrease in B-cell-mediated IgH production. Ibrutinib and its analogs Acalabrutinib and Zanubrutinib selectively inhibit Bruton's tyrosine kinase (BTK), a key molecule in the B-cell receptor (BCR) signaling pathway. By impairing BCR signaling, these inhibitors reduce the proliferation and survival of B-cells, with a consequent reduction in IgH output. Fostamatinib disrupts BCR signaling by inhibiting spleen tyrosine kinase (Syk), which then diminishes B-cell activity and decreases the production of IgH. Venetoclax selectively targets BCL-2, an anti-apoptotic protein, thereby promoting apoptosis in B-cells and reducing the number of B-cells capable of producing IgH. Each of these chemical inhibitors acts on different signaling components that are intricately involved in the regulation of B-cell growth, activation, differentiation, or survival, thereby modulating the levels and function of IgH.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Cyclosporin A | 59865-13-3 | sc-3503 sc-3503-CW sc-3503A sc-3503B sc-3503C sc-3503D | 100 mg 100 mg 500 mg 10 g 25 g 100 g | $63.00 $92.00 $250.00 $485.00 $1035.00 $2141.00 | 69 | |
Cyclosporin A binds to the cytosolic protein cyclophilin of immunocompetent lymphocytes, especially T-lymphocytes. This complex of cyclosporin A and cyclophilin inhibits calcineurin, which under normal circumstances induces the transcription of interleukin-2. Interleukin-2 is a key cytokine that triggers the proliferation of T- and B-cells, the latter of which is responsible for the production of immunoglobulins including IgH. By inhibiting this signal transduction pathway, Cyclosporin A functionally inhibits the activation of B-cells and therefore the production of IgH. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin forms a complex with FKBP12, and this complex binds to mTOR Complex 1 (mTORC1), inhibiting its activity. mTORC1 is involved in the regulation of cell growth, proliferation, and survival. By inhibiting mTORC1, Rapamycin can reduce the proliferation of B-cells and the subsequent production and activity of IgH due to a decrease in B-cell activation and differentiation. | ||||||
CAL-101 | 870281-82-6 | sc-364453 | 10 mg | $193.00 | 4 | |
Idelalisib selectively inhibits the delta isoform of the enzyme phosphoinositide 3-kinase (PI3K), which is expressed in hematopoietic cells. PI3K-delta signaling is important for the activation, proliferation, and survival of B-cells. Inhibition of PI3K-delta by Idelalisib leads to reduced B-cell proliferation and survival, thereby decreasing the production and function of IgH. | ||||||
Ibrutinib | 936563-96-1 | sc-483194 | 10 mg | $156.00 | 5 | |
Ibrutinib is an inhibitor of Bruton's tyrosine kinase (BTK). BTK is essential for B-cell receptor (BCR) signaling, which plays a crucial role in B-cell development, activation, and signaling. By inhibiting BTK, Ibrutinib impairs BCR signaling, leading to reduced B-cell proliferation and survival, with a consequent decrease in the production and function of IgH. | ||||||
R788 | 901119-35-5 | sc-364597 sc-364597A | 2 mg 50 mg | $405.00 $4000.00 | 2 | |
R788 inhibits spleen tyrosine kinase (Syk), which is involved in B-cell receptor (BCR) signaling. BCR signaling is critical for B-cell activation and proliferation. By inhibiting Syk, R788 disrupts BCR signaling, resulting in reduced B-cell activity and a decrease in IgH production and function. | ||||||
Acalabrutinib | 1420477-60-6 | sc-507392 | 250 mg | $255.00 | ||
Acalabrutinib selectively inhibits Bruton's tyrosine kinase (BTK), which plays a significant role in B-cell receptor (BCR) signaling. Inhibition of BTK by Acalabrutinib leads to reduced BCR signaling, thereby decreasing B-cell activation, proliferation, and survival, ultimately diminishing the production and function of IgH. | ||||||
ABT-199 | 1257044-40-8 | sc-472284 sc-472284A sc-472284B sc-472284C sc-472284D | 1 mg 5 mg 10 mg 100 mg 3 g | $118.00 $337.00 $520.00 $832.00 $1632.00 | 10 | |
ABT-199 is a selective inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 allows cancerous B-cells to survive. By inhibiting BCL-2, ABT-199 promotes apoptosis in these cells, thereby reducing the number of B-cells available to produce and secrete IgH. | ||||||
IPI 145 | 1201438-56-3 | sc-488318 | 5 mg | $317.00 | ||
Duvelisib inhibits both the gamma and delta isoforms of phosphoinositide 3-kinase (PI3K), which are involved in the activation and viability of B-cells. By inhibiting PI3K, Duvelisib impairs B-cell receptor signaling, leading to reduced survival and proliferation of B-cells and a consequent decrease in IgH production and function. | ||||||
Zanubrutinib | 1691249-45-2 | sc-507434 | 5 mg | $360.00 | ||
Zanubrutinib is a Bruton's tyrosine kinase (BTK) inhibitor. It impairs B-cell receptor signaling, which is critical for B-cell proliferation and survival. By inhibiting BTK, Zanubrutinib limits B-cell activity, resulting in a reduction of IgH production and function. | ||||||