目录号 | 产品详情 | 靶点 | |
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T63810 | |||
BTK-IN-7 是选择性的、有效的 BTK 抑制剂,其 IC50 值为 4.0 nM。BTK-IN-7 在酶 (ITK>250-fold, EGFR>2500-fold) 和细胞水平 (ITK>227-fold,EGFR27-fold) 都表现出较高的选择性。BTK-IN-7 表现出较高的抗肿瘤作用。 | |||
T79113 | BTK | ||
BTK-IN-25(compound 71)作为BTK抑制剂,展现出对BTK(C481S)的强效抑制作用,IC50为0.77 nM。该化合物在DOHH2细胞中对BTK亦表现出高效抑制,IC50为1 nM。 | |||
T63173 | |||
BTK-IN-8 是一种有效的、选择性的、外周共价 BTK 抑制剂,其 IC50 值为 0.22 nM,Kd 值为 0.91 nM。BTK-IN-8 表现出良好的全血 CD69 细胞效力,其 IC50 值为 0.029 μM。 | |||
T1835 | Tyrosine Kinases Src BTK Ligands for Target Protein for PROTAC | ||
Ibrutinib (PCI-32765) 是一种不可逆的、选择性的 Btk 抑制剂,IC50=0.5 nM,它是一种 Btk 配体,用于合成一系列 PROTAC 分子,如 P13I。P13I 作用于人 Burkitt’s 淋巴瘤 RAMOS 细胞,浓度为 10 和 100 nM 时,分别降解 73% 和 89% Btk。 | |||
T73275 | |||
BTK-IN-22 是一种BTK 抑制剂 (IC50: 12.8 nM)。BTK-IN-22 还抑制 BLX 和 BMX,IC50分别为 35.6 和 5.7 nM。与 Ibrutinib 相比,BTK-IN-22 显示出更高的激酶选择性。 | |||
T63254 | |||
BTK-IN-11 是 BTK 的有效抑制剂。其中 BTK 在分别由 B 细胞和骨髓细胞中的 B 细胞抗原受体 (BCR) 和 Fcγ 受体 (FcγR) 介导的信号传导中起重要作用。BTK-IN-11 对自身免疫性疾病、炎症性疾病或癌症相关疾病表现出研究潜力。 | |||
T73276 | |||
BTK-IN-23 是一种BTK 抑制剂 (IC50: 12.8 nM)。BTK-IN-23 还抑制 BLX 和 BMX,IC50分别为 35.6 和 5.7 nM。与 Ibrutinib 相比,BTK-IN-23 显示出更高的激酶选择性。 | |||
T62716 | |||
BTK-IN-10 是一种 BTK 的有效抑制剂,能够作用于野生型 BTK (IC50<5 nM) 或突变型 BTK (C481S) (IC50<5 nM)。 | |||
T63182 | |||
BTK-IN-15 是一种新型的、口服具有活力的布鲁顿酪氨酸激酶 (BTK) 抑制剂,能够抑制 BTK (IC50: 0.7 nM)。BTK-IN-15 可诱导癌细胞凋亡,具有良好的激酶选择性和抗肿瘤活性。 | |||
T73303 | |||
BTK-IN-17是一种选择性且具有BTK 抑制剂,IC50值为 13.7 nM。BTK-IN-17 降低 p-BTKY223和 p-PLCγ2Y1217的表达。BTK-IN-17 具有抗炎作用。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-02271 | BTK Protein, Human, Recombinant (His) | Human | Baculovirus | ||
Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling. Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately leads to B-cell activation. After BCR engagement and activation at the plasma membrane, phosphorylates PLCG2 at several sites, igniting the downstream signaling pathway through calcium mobilization, followed by activation of the protein kinase C (PKC) family members. PLCG2 phosphorylation is performed in close cooperation with the adapter protein B-cell linker protein BLNK. BTK acts as a platform to bring together a diverse array of signaling proteins and is implicated in cytokine receptor signaling pathways. Plays an important role in the function of immune cells of innate as well as adaptive immunity, as a component of the Toll-like receptors (TLR) pathway. The TLR pathway acts as a primary surveillance system for the detection of pathogens and are crucial to the activation of host defense. Especially, is a critical molecule in regulating TLR9 activation in splenic B-cells. Within the TLR pathway, induces tyrosine phosphorylation of TIRAP which leads to TIRAP degradation. BTK plays also a critical role in transcription regulation. Induces the activity of NF-kappa-B, which is involved in regulating the expression of hundreds of genes. BTK is involved on the signaling pathway linking TLR8 and TLR9 to NF-kappa-B. Transiently phosphorylates transcription factor GTF2I on tyrosine residues in response to BCR. GTF2I then translocates to the nucleus to bind regulatory enhancer elements to modulate gene expression. ARID3A and NFAT are other transcriptional target of BTK. BTK is required for the formation of functional ARID3A DNA-binding complexes. There is however no evidence that BTK itself binds directly to DNA. BTK has a dual role in the regulation of apoptosis.
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TMPY-04570 | ITK Protein, Mouse, Recombinant (aa 351-619, His & GST) | Mouse | Baculovirus-Insect Cells | ||
IL-2-inducible T cell kinase is a member of the protein kinase superfamily, Tyr protein kinase family, and TEC subfamily. It contains 1 Btk-type zinc finger, 1 PH domain, 1 protein kinase domain, 1 SH2 domain, and 1 SH3 domain. As an intracellular kinase expressed in T-cells, IL-2-inducible T cell kinase contains both SH2 and SH3 domains which are often found in intracellular kinases. It is thought to play a role in T-cell proliferation and differentiation. It regulates the development, function, and differentiation of conventional T-cells and nonconventional NKT-cells. IL-2-inducible T cell kinase also plays an essential role in the regulation of the adaptive immune response. Effects in IL-2-inducible T cell kinase are the cause of lymphoproliferative syndrome EBV-associated autosomal type 1 (LPSA1). LPSA1 is a rare immunodeficiency characterized by extreme susceptibility to infection with Epstein-Barr virus (EBV). Inadequate immune response to EBV can have a fatal outcome. Clinical features include splenomegaly, lymphadenopathy, anemia, thrombocytopenia, pancytopenia, recurrent infections. There is an increased risk of lymphoma.
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TMPY-05249 | ITK Protein, Human, Recombinant (Actived By LCK, GST) | Human | Baculovirus-Insect Cells | ||
IL-2-inducible T cell kinase is a member of the protein kinase superfamily, Tyr protein kinase family, and TEC subfamily. It contains 1 Btk-type zinc finger, 1 PH domain, 1 protein kinase domain, 1 SH2 domain, and 1 SH3 domain. As an intracellular kinase expressed in T-cells, IL-2-inducible T cell kinase contains both SH2 and SH3 domains which are often found in intracellular kinases. It is thought to play a role in T-cell proliferation and differentiation. It regulates the development, function, and differentiation of conventional T-cells and nonconventional NKT-cells. IL-2-inducible T cell kinase also plays an essential role in the regulation of the adaptive immune response. Effects in IL-2-inducible T cell kinase are the cause of lymphoproliferative syndrome EBV-associated autosomal type 1 (LPSA1). LPSA1 is a rare immunodeficiency characterized by extreme susceptibility to infection with Epstein-Barr virus (EBV). Inadequate immune response to EBV can have a fatal outcome. Clinical features include splenomegaly, lymphadenopathy, anemia, thrombocytopenia, pancytopenia, recurrent infections. There is an increased risk of lymphoma.
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TMPH-02962 | Lyn Protein, Mouse, Recombinant (His & Myc) | Mouse | E. coli | ||
Non-receptor tyrosine-protein kinase that transmits signals from cell surface receptors and plays an important role in the regulation of innate and adaptive immune responses, hematopoiesis, responses to growth factors and cytokines, integrin signaling, but also responses to DNA damage and genotoxic agents. Functions primarily as negative regulator, but can also function as activator, depending on the context. Required for the initiation of the B-cell response, but also for its down-regulation and termination. Plays an important role in the regulation of B-cell differentiation, proliferation, survival and apoptosis, and is important for immune self-tolerance. Acts downstream of several immune receptors, including the B-cell receptor, CD79A, CD79B, CD5, CD19, CD22, FCER1, FCGR2, FCGR1A, TLR2 and TLR4. Plays a role in the inflammatory response to bacterial lipopolysaccharide. Mediates the responses to cytokines and growth factors in hematopoietic progenitors, platelets, erythrocytes, and in mature myeloid cells, such as dendritic cells, neutrophils and eosinophils. Acts downstream of EPOR, KIT, MPL, the chemokine receptor CXCR4, as well as the receptors for IL3, IL5 and CSF2. Plays an important role in integrin signaling. Regulates cell proliferation, survival, differentiation, migration, adhesion, degranulation, and cytokine release. Down-regulates signaling pathways by phosphorylation of immunoreceptor tyrosine-based inhibitory motifs (ITIM), that then serve as binding sites for phosphatases, such as PTPN6/SHP-1, PTPN11/SHP-2 and INPP5D/SHIP-1, that modulate signaling by dephosphorylation of kinases and their substrates. Phosphorylates LIME1 in response to CD22 activation. Phosphorylates BTK, CBL, CD5, CD19, CD72, CD79A, CD79B, CSF2RB, DOK1, HCLS1, LILRB3/PIR-B, MS4A2/FCER1B, SYK and TEC. Promotes phosphorylation of SIRPA, PTPN6/SHP-1, PTPN11/SHP-2 and INPP5D/SHIP-1. Required for rapid phosphorylation of FER in response to FCER1 activation. Mediates KIT phosphorylation. Acts as an effector of EPOR (erythropoietin receptor) in controlling KIT expression and may play a role in erythroid differentiation during the switch between proliferation and maturation. Depending on the context, activates or inhibits several signaling cascades. Regulates phosphatidylinositol 3-kinase activity and AKT1 activation. Regulates activation of the MAP kinase signaling cascade, including activation of MAP2K1/MEK1, MAPK1/ERK2, MAPK3/ERK1, MAPK8/JNK1 and MAPK9/JNK2. Mediates activation of STAT5A and/or STAT5B. Phosphorylates LPXN on 'Tyr-72'. Kinase activity facilitates TLR4-TLR6 heterodimerization and signal initiation. Phosphorylates SCIMP on 'Tyr-96'; this enhances binding of SCIMP to TLR4, promoting the phosphorylation of TLR4, and a selective cytokine response to lipopolysaccharide in macrophages. Phosphorylates CLNK.
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