Silmitasertib | CK2 inhibitor

CAS:
 1009820-21-6
Catalog Number:
 10-4809
cx4945 chemical structure

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Silmitasertib (1009820-21-6) is a potent and orally bioavailable inhibitor of casein kinase 2 (Ki=0.38 nM) acting at the ATP-binding site.1 It has been in preclinical and clinical development for a variety of cancers.2 It inhibits CK2-mediated phosphorylation of the SALL2 tumor suppressor preventing its proteasomal degradation and induces cell death in a variety of tumor cell lines.3 It inhibits fibroblast-like synoviocytes reducing rheumatoid arthritis disease severity in rodent models4 and inhibits collagen degradation5.

References/Citations:

  1. Siddiqui-Jain et al. (2010), CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy; Cancer Res. 70 10288
  2. Sol Lee et al. (2024), CX-4945 (Silmitasertib) Induces Cell Death by Impairing Lysosomal Utilization in KRAS Mutant Cholangiocarcinoma Cell Lines; Anticancer Res. 44 1939
  3. Hermosilla et al. (2024), Casein kinase 2 phosphorylates and induces the SALL2 tumor suppressor degradation in colon cancer cells; Cell Death Dis. 15 223
  4. Luo et al. (2023), CX-4945 inhibits fibroblast-like synoviocytes functions through the CK2-p53 axis to reduce rheumatoid arthritis disease severity; Int. Immunopharmacol. 119 110163
  5. Jeon and Lee. (2023), CK2 inhibitor CX4945 inhibits collagen degradation of HaCaT human keratinocyte cells via attenuation of MMP-1 secretion; Mol. Biol. Rep. 50 9691
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CAS:
1009820-21-6
Catalog Number:
10-4809
Activity:
CK2 inhibitor
Chemical Names:
5-[(3-Chlorophenyl)amino]-benzo[c]-2,6-naphthyridine-8-carboxylic acid
Alternate Name:
CX-4945
Molecular Weight:
349.77
Molecular Formula:

C19H12ClN3O2

Solubility:
Soluble in DMSO (30 mg/ml)
Physical Properties:
Beige solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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Silmitasertib (1009820-21-6) is a potent and orally bioavailable inhibitor of casein kinase 2 (Ki=0.38 nM) acting at the ATP-binding site.1 It has been in preclinical and clinical development for a variety of cancers.2 It inhibits CK2-mediated phosphorylation of the SALL2 tumor suppressor preventing its proteasomal degradation and induces cell death in a variety of tumor cell lines.3 It inhibits fibroblast-like synoviocytes reducing rheumatoid arthritis disease severity in rodent models4 and inhibits collagen degradation5.

References/Citations:

  1. Siddiqui-Jain et al. (2010), CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy; Cancer Res. 70 10288
  2. Sol Lee et al. (2024), CX-4945 (Silmitasertib) Induces Cell Death by Impairing Lysosomal Utilization in KRAS Mutant Cholangiocarcinoma Cell Lines; Anticancer Res. 44 1939
  3. Hermosilla et al. (2024), Casein kinase 2 phosphorylates and induces the SALL2 tumor suppressor degradation in colon cancer cells; Cell Death Dis. 15 223
  4. Luo et al. (2023), CX-4945 inhibits fibroblast-like synoviocytes functions through the CK2-p53 axis to reduce rheumatoid arthritis disease severity; Int. Immunopharmacol. 119 110163
  5. Jeon and Lee. (2023), CK2 inhibitor CX4945 inhibits collagen degradation of HaCaT human keratinocyte cells via attenuation of MMP-1 secretion; Mol. Biol. Rep. 50 9691

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