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Cat. No. | Product Name | Target | Signaling Pathways |
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T26817 |
Bim-BLK-A
Bim Blocker A,Compound A,Bim BLK A,BimBLKA |
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Bim-BLK-A efficiently blocks Bim-induced apoptosis after Bax is activated on the mitochondria. The cellular target of Bim-BLK-A was identified to be the succinate dehydrogenase subunit B (SDHB) protein of complex II of the mitochondrial electron transfer | |||
T73366 |
BLK-IN-2
|
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BLK-IN-2为一种高效、选择性且不可逆的B-淋巴酪氨酸激酶(BLK)抑制剂,具有5.9 nM的IC50值。该化合物亦能抑制BTK,其IC50值为202.0 nM。BLK-IN-2在多种淋巴瘤细胞中展现出显著的抗增殖作用。 | |||
T63959 |
BLK-IN-1
|
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BLK-IN-1 是一种选择性的、共价的 B-淋巴酪氨酸激酶 (BLK) 和 BTK 抑制剂,他们的 IC50 值分别为 18.8 nM 和 20.5 nM。BLK-IN-1 能够用于研究癌症。 | |||
T9072 |
Tuxobertinib
BDTX-189 |
EGFR; HER; BTK; RIP kinase | Angiogenesis; Apoptosis; JAK/STAT signaling; NF-κB; Tyrosine Kinase/Adaptors |
Tuxobertinib (BDTX-189) 是一种高效可口服的选择性 EGFR 和 HER2变构突变抑制剂,具有抗癌活性。它对 EGFR、HER2、BLK 和 RIPK2 的 KD 值分别为 0.2、0.76、13 和 1.2 nM。 | |||
T6078 |
Saracatinib
AZD0530,塞卡替尼 |
EGFR; Src; BTK; Autophagy | Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Saracatinib (AZD0530) 是一种有效的 Src 抑制剂,抑制 c-Src、Lck、c-YES、Lyn、Fyn、Fgr 和 Blk 的 IC50值在 2.7 到 11 nM 之间,对其他酪氨酸激酶具有选择性。 | |||
T14692 |
BMX-IN-1
BMX kinase inhibitor |
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
BMX-IN-1 (BMX kinase inhibitor) 是 X 染色体上的骨髓酪氨酸激酶 (BMX, IC50 = 8 nM) 和相关的布鲁顿酪氨酸激酶 (BTK, IC50 = 10.4 nM) 的特异性抑制剂,但 BMX-IN-1 对 Blk、JAK3、EGFR、Itk 或 Tec 活性的效力要低 47-656 倍以上。 | |||
T71819 |
RK-20448
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RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R, and Tie-2. It also inhibits BLK, Csk, Fyn, and Lyn. RK-20448 is the cis isomer of A-419259 | |||
T39129 |
BMS-986143
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BMS-986143 是一种口服有效的、可逆的BTK 抑制剂,IC50为 0.26 nM,具有自身免疫性疾病的研究潜力。BMS-986143 还抑制 TEC、BLK、BMX、TXK FGR、YES1、ITK,IC50分别为 3 nM、5 nM、7 nM、10 nM、15 nM、19 nM、21 nM。 | |||
T74642 |
DB1113
|
PROTACs | PROTAC |
DB1113 (Example 24) 是一种靶向蛋白激酶降解的双功能化合物。DB1113 可降解 ABL1,ABL2,BLK,CDK11B,CDK4,CSK,EPHA3,FER,GAK,LIMK1,MAP3K20,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK3,NLK,PDIK1L,PTK2B,RIPK1,RPS6KA1,RPS6KA3,SIK2,SIK3,STK35,TNK2 和 ULK1。DB1113 可用于研究异常激酶活性介导的疾病或紊乱。 | |||
T7819 |
TAS0728
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EGFR; HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
TAS0728 是一种 HER2 抑制剂,与HER2的 C805 位点共价结合,IC50值为 13 nM。它抑制 HER2、HER3 及其下游效应蛋白的磷酸化,具有抗肿瘤活性。 | |||
T10802 |
CHMFL-EGFR-202
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EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
CHMFL-EGFR-202 是一种有效、不可逆的表皮生长因子受体 (EGFR) 突变型激酶抑制剂, 对耐药突变型 EGFR T790M 和 WT EGFR 激酶作用的 IC50 分别为 5.3 nM 和 8.3 nM。 | |||
T74644 |
DB0614
|
PROTACs | PROTAC |
DB1113 (Example 24) 是一种靶向蛋白激酶降解的双功能化合物。DB1113 可降解ABL1,ABL2,BLK,CDK11B,CDK4,CSK,EPHA3,FER,GAK,LIMK1,MAP3K20,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK3,NLK,PDIK1L,PTK2B,RIPK1,RPS6KA1,RPS6KA3,SIK2,SIK3,STK35,TNK2 和ULK1。DB1113 可用于研究异常激酶活性介导的疾病或紊乱。 | |||
T5138 |
BMS-986142
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BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
BMS986142 是一种有效的、具有高选择性的 Bruton's 酪氨酸激酶 (BTK)可逆性抑制剂 (IC50:0.5 nM)。 | |||
T1835 |
Ibrutinib
伊布替尼,依鲁替尼,PCI-32765 |
Tyrosine Kinases; Src; BTK; Ligands for Target Protein for PROTAC | Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors |
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。 | |||
T12542 |
Rilzabrutinib
PRN1008 |
EGFR; Others; HER; BTK | Angiogenesis; JAK/STAT signaling; Others; Tyrosine Kinase/Adaptors |
Rilzabrutinib (PRN1008) 是一种可逆的、选择性的、有口服活性的布鲁顿氏酪氨酸激酶(BTK)共价抑制剂,其 IC50=1.3 nM。 | |||
T13564L |
AZ7550 hydrochloride
AZ7550 hydrochloride (1421373-99-0 free base) |
EGFR; IGF-1R | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
AZ7550 hydrochloride (AZ7550 hydrochloride ) 是 AZD9291 的活性代谢物,可抑制 IGF1R 活性,IC50为 1.6 μM。 | |||
T13564 |
AZ7550
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MLK; FAK; EGFR; FLT; Tyrosine Kinases; PYK2; MNK; IGF-1R; ACK; BTK; ALK; Drug Metabolite | Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; Metabolism; Tyrosine Kinase/Adaptors |
AZ7550 是 AZD9291 的活性代谢物,可抑制 IGF1R 活性,IC50为 1.6 μM。 | |||
T16578 |
PRN694
|
Others | Others |
PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting ly | |||
T10801 |
CHMFL-ABL/KIT-155
CHMFL-ABL-KIT-155 |
c-Kit | Tyrosine Kinase/Adaptors |
CHMFL-ABL/KIT-155 is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s: 46 nM/75 nM). It arrests cell cycle progression and induces apoptosis. | |||
T18049 |
Ibrutinib-biotin
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Others | Others |
Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, has an IC50 of 0.755-1.02 nM for BTK. |
Cat. No. | Product Name | Species | Expression System |
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TMPJ-00307 |
BLK Protein, Human, Recombinant (His)
Tyrosine-Protein Kinase Blk,BLK,B Lymphocy... |
Human | E. coli |
Tyrosine-Protein Kinase Blk (BLK) contains one protein kinase domain, one SH2 domain and one SH3 domain. BLK is a non-receptor tyrosine kinase, which is involved in B-lymphocyte development, differentiation and signaling. B-cell receptor (BCR) signaling requires a tight regulation of several protein tyrosine kinases and phosphatases, and associated coreceptors. Signaling through BLK plays an important role in transmitting signals through surface immunoglobulines and supports the pro-B to pre-B t... | |||
TMPY-04388 |
BLK Protein, Human, Recombinant (GST)
MODY11,BLK proto-oncogene, Src family tyrosine kina... |
Human | Baculovirus Insect Cells |
Tyrosine-protein kinase Blk, also known as B lymphocyte kinase, p55-Blk and BLK, is a member of theprotein kinase superfamily, Tyr protein kinase family and SRC subfamily. BLK / p55-Blk is expressed in lymphatic organs, pancreatic islets, Leydig cells, striate ducts of salivary glands and hair follicles. BLK / p55-Blk is a src-family protein tyrosine kinase specifically expressed in B-lineage cells of mice. The early onset of Blk expression during B-cell development in the bone marrow and... |