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Ack1 (TNK2)
ACK1 (also known as activated Cdc42-associated kinase 1 or TNK2) is a cytosolic effecter of activated transmembrane receptor tyrosine kinases (RTKs), wherein it shuttles between the cytosol and the nucleus to rapidly transduce extracellular signals from the RTKs to the intracellular effectors, recent data unfold a new aspect of its functionality as an epigenetic regulator. ACK1 gene encodes a large protein of 1038 amino acids (140 kDa) that is post-translationally modified by multiple tyrosine phosphorylations that regulate its kinase activation. The multi-domain structure of ACK1 sets it apart from other non-receptor tyrosine kinases and includes at least 8 distinct domains; the Sterile alpha motif (SAM), kinase or catalytic domain, SH3 domain, GTPase binding domain (also known as Cdc42-binding domain or CRIB domain), Clathrin interacting region, PPXY motif or WW domain interacting region, a MIG6 homology region (MHR), also known as EGFR binding domain and an ubiquitin-association (UBA) domain.
ACK1 interacts with the Estrogen Receptor (ER)/histone demethylase KDM3A (JHDM2a) complex, modifies KDM3A by tyrosine phosphorylation to regulate transcriptional outcome at HOXA1 locus to promote the growth of tamoxifen-resistant breast cancer. It is also well established that ACK1 regulates the activity of Androgen Receptor (AR) by tyrosine phosphorylation to fuel the growth of hormone-refractory prostate cancers. Further, recent explosion in genomic sequencing has revealed recurrent ACK1 gene amplification and somatic mutations in a variety of human malignancies, providing a molecular basis for its role in neoplastic transformation.With the accelerated development of potent and selective ACK1 inhibitors, targeted treatment for cancers harboring aberrant ACK1 activity may soon become a clinical reality.
References:
1.Mahajan K,et al. Oncogene. 2015 Aug 6;34(32):4162-7.
ACK1 interacts with the Estrogen Receptor (ER)/histone demethylase KDM3A (JHDM2a) complex, modifies KDM3A by tyrosine phosphorylation to regulate transcriptional outcome at HOXA1 locus to promote the growth of tamoxifen-resistant breast cancer. It is also well established that ACK1 regulates the activity of Androgen Receptor (AR) by tyrosine phosphorylation to fuel the growth of hormone-refractory prostate cancers. Further, recent explosion in genomic sequencing has revealed recurrent ACK1 gene amplification and somatic mutations in a variety of human malignancies, providing a molecular basis for its role in neoplastic transformation.With the accelerated development of potent and selective ACK1 inhibitors, targeted treatment for cancers harboring aberrant ACK1 activity may soon become a clinical reality.
References:
1.Mahajan K,et al. Oncogene. 2015 Aug 6;34(32):4162-7.
Tyrosine Kinase
Ack1 (TNK2)
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(R)-9bMS
产品货号 : M16923
cas no: ——
(R)-9bMS 是一种有效的选择性 ACK1 (TNK2) 抑制剂，IC50 为 48 nM。
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AIM-100
产品货号 : M16349
cas no: 873305-35-2
AIM-100 (AIM100) 是一种高效的 Ack1 (TNK2) 抑制剂 (IC50=24 nM)，对 Ack1 的选择性高于 ABL1、BTK、Lck 和 LYN。
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XMD16-5
产品货号 : M11379
cas no: 1345098-78-3
XMD16-5 是一种有效的 Ack1 (TNK2) 抑制剂，ELISA 测定中 IC50 为 0.38 uM。
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XMD8-87
产品货号 : M10934
cas no: 1234480-46-6
XMD8-87（Ack1 抑制剂 B19）是一种有效的 Ack1 抑制剂，Kd 为 15 nM，在 2 uM 浓度时可抑制 HEK293 细胞中 EGF 诱导的自身磷酸化。
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Ack1 inhibitor 37
产品货号 : M10126
cas no: 1026493-77-5
Ack1抑制剂37是一种有效的选择性Ack1 (TNK2)抑制剂，Ki为0.3 nM。
