c-abl-in-1

C-ABL-IN-1 is a new and specific inhibitor of the c-Abl protein, which effectively prevents the progression of neurodegeneration observed in Parkinson's disease.

OSI-930 是 Kit，KDR 和 CSF-1R (c-Fms)的口服选择性抑制剂，IC50分别为 80 nM，9 nM 和 15 nM。它具有抗肿瘤活性，靶向肿瘤中的癌细胞增殖和血管生成。它还适度抑制 Flt-1，c-Raf 和 Lck，并且对 PDGFRα β，Flt-3和 Abl 具有较弱的抑制活性。

cSRC BCR-ABL-IN-1 (compound 21b) 是一种强效Bcr-Abl和C-Src酶抑制剂，其对Bcr-Abl和C-Src的半数抑制浓度（IC50）分别为56.2 nM和101 nM。此外，cSRC BCR-ABL-IN-1 具有细胞毒性。

C-ABL-IN-2 is a highly effective inhibitor of the c-Abl protein, which plays a significant role in the development of several diseases, including cancer. This compound exhibits promise for investigating neurodegenerative disorders such as amyotrophic lateral sclerosis (ALS) and Parkinson's disease (PD), as well as cancer. (Source: WO2020260871A1, compound 25) [1].

c-ABL-IN-3, a highly effective c-Abl inhibitor, exhibits promising potential for studying neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS) and Parkinson's disease (PD), as well as cancer [1]. The activation of c-Abl has been strongly implicated in a range of diseases, notably cancer [1]. It offers valuable opportunities for research in these fields [1].

Imatinib Impurity E 是 Imatinib 的杂质。Imatinib 是一种口服生物可用的酪氨酸激酶抑制剂，可选择性抑制 BCR ABL，v-Abl，PDGFR，c-kit 激酶活性。Imatinib (STI571) 靠近 ATP 结合位点结合，将其锁定在封闭或自我抑制的构象中，因此半竞争性抑制蛋白质的酶活性。Imatinib 还抑制 SARS-CoV 和MERS-CoV。

c-ABL-IN-5是一种选择性c-Abl抑制剂，具有神经保护功能。该化合物显示出血脑屏障渗透性、代谢稳定性和优良的药物动力学特性。经[18F]标记的c-ABL-IN-5（化合物[18F]3）可用作PET示踪剂，以评估疾病改善的功效。此外，c-ABL-IN-5适用于帕金森病（PD）等神经退行性疾病的研究。

Protein kinase D (PKD), a serine threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

GNF-6 (Compound 14) 抑制 BCR-ABL-T315I 的门控苏氨酸残基突变，对 c-ABL-T334I、BCR-ABL 和 BCR-ABL-T315I 变体的 IC50 值分别为 0.25 μM、0.09 μM 和 0.590 μM。GNF-6 是一种 ATP 竞争性抑制剂，通过破坏疏水性脊柱 (疏水性相互作用网络) 的组装，使激酶保持在非活性“DFG-out”构象中。