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AdipoGen Life Sciences
CRT0066101 . HCl
50
CHF
CHF 50.00
In stock
AG-CR1-3550-M0011 mgCHF 50.00
| Product Details | |
|---|---|
| Synonyms | 2-[4-[[(2R)-2-Aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)-phenol . hydrochloride |
| Product Type | Chemical |
| Properties | |
| Formula |
C18H22N6O . 3HCl |
| MW | 338.4 . 109.4 |
| CAS | 1781742-22-0 |
| Purity Chemicals | ≥98% |
| Appearance | White to off-white solid. |
| Solubility | Soluble in water (10mg/ml) or DMSO (3mg/ml). |
| InChi Key | HWZPJKPBOZVLEB-XJCLVHIMSA-N |
| Smiles | N[C@@H](CN([H])C1=CC=NC(C2=C(C=CC(C3=CN(N=C3)C)=C2)O)=N1)CC.Cl.Cl.Cl |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Protect from light when in solution. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
- CRT0066101 is an inhibitor of all three PKD isoforms (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2 and PKD3, respectively). It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src and c-Abl.
- PKD family members play an important role in regulating several cellular processes and activities, including chromatin organization, Golgi function, gene expression, cell survival, adhesion, motility, differentiation, DNA synthesis and proliferation.
- CRT0066101 shows anticancer activity by blocking cell proliferation, inducing apoptosis, G2/M phase arrest, inhibiting migration and invasion and reducing the viability of several cancer cells both in vitro and in vivo.
- CRT0066101 reduced PKD-dependent NF-κB activation and NF-κB-dependent gene expressions in pancreatic cancer cells in vitro and showed antiviral activities inhibiting viral RNA replication and viral protein expression.
- Protein kinase D (PKD) has emerged as an important NLRP3 kinase that catalyzes the release of a phosphorylated NLRP3 species that is competent for inflammasome complex assembly. PKD inhibitor CRT0066101 could block NLRP3 inflammasome assembly and interleukin-1β production.
- CRT0066101 also inhibits MyD88 and TLR4 expression and reduces NF-κB, ERK and JNK phosphorylation, indicating that it exerts anti-inflammatory effects on LPS-induced inflammation through the TLR4/MyD88 signaling pathway.
Product References
- A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo: K.B. Harikumar, et al.; Mol. Cancer Ther. 9, 1136 (2010)
- Protein kinase D1 promotes anchorage-independent growth, invasion, and angiogenesis by human pancreatic cancer cells: N. Ochi, et al.; J. Cell Physiol. 226, 1074 (2011)
- Protein kinase d regulates cell death pathways in experimental pancreatitis: J. Yuan, et al.; Front. Physiol. 3, 60 (2012)
- Protein kinase d as a potential chemotherapeutic target for colorectal cancer: N. Wei, et al.; Mol. Cancer Ther. 13, 1130 (2014)
- Effective Targeting of Estrogen Receptor-Negative Breast Cancers with the Protein Kinase D Inhibitor CRT0066101: S. Borges, et al.; Mol. Cancer Ther. 14, 1306 (2015)
- Novel Small Molecule Inhibitors of Protein Kinase D Suppress NF-kappaB Activation and Attenuate the Severity of Rat Cerulein Pancreatitis: J. Yuan, et al.; Front. Physiol. 8, 1014 (2017)
- Investigation of the Role of Protein Kinase D in Human Rhinovirus Replication: A. Guedan, et al.; J. Virol. 91, e00217 (2017)
- Protein kinase D at the Golgi controls NLRP3 inflammasome activation: Z. Zhang, et al.; J. Exp. Med. 214, 2671 (2017)
- Developments in the Discovery and Design of Protein Kinase D Inhibitors: P. Gilles, et al.; ChemMedChem 16, 2158 (2021) (Review)
- Evaluation of protein kinase D auto-phosphorylation as biomarker for NLRP3 inflammasome activation: D. Heiser, et al.; PLoS One 16, e0248668 (2021)
- Small molecule inhibitor CRT0066101 inhibits cytokine storm syndrome in a mouse model of lung injury: B. Cui, et al.; Int. Immunopharmacol. 120, 110240 (2023)