Drug Information

Drug (ID: DG00248) and It's Reported Resistant Information

• Name: Isoarnebin 4
• Synonyms: Shikonin; NSC 252844; Shikonin S; Shikonin,(S); Tokyo Violet
• Indication:
  In total 1 Indication(s)
  COVID-19 [ICD-11: 1D92]; Investigative; [1]
• Target: COVID-19 papain-like proteinase (PL-PRO); R1AB_SARS2 (819-2763); [1]
• Formula: C16H16O5
• IsoSMILES: CC(=CC[C@H](C1=CC(=O)C2=C(C=CC(=C2C1=O)O)O)O)C
• InChI: 1S/C16H16O5/c1-8(2)3-4-10(17)9-7-13(20)14-11(18)5-6-12(19)15(14)16(9)21/h3,5-7,10,17-19H,4H2,1-2H3/t10-/m1/s1
• InChIKey: NEZONWMXZKDMKF-SNVBAGLBSA-N
• PubChem CID: 479503
• ChEBI ID: CHEBI:81068
• TTD Drug ID: D0QM4U

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Brain cancer [ICD-11: 2A00]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: hsa-mir-143 [1]

• Molecule Alteration: Expression; Up-regulation
• Sensitive Disease: Glioblastoma [ICD-11: 2A00.02]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell apoptosis; Activation; hsa04210
• Cell Pathway Regulation: Cell proliferation; Inhibition; hsa05200
• Cell Pathway Regulation: Mitochondrial apoptotic signaling pathway; Activation; hsa04210
• In Vitro Model: GBM cells; Brain; Homo sapiens (Human); N.A.
• In Vivo Model: Mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: qRT-PCR
• Experiment for Drug Resistance: CCK8 assay; Flow cytometry assay
• Mechanism Description: miR-143 enhances the antitumor activity of shikonin by targeting BAG3 and reducing its expression in human glioblastoma stem cell.

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: BAG family molecular chaperone regulator 3 (BAG3) [1]

• Molecule Alteration: Expression; Down-regulation
• Sensitive Disease: Glioblastoma [ICD-11: 2A00.02]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell apoptosis; Activation; hsa04210
• Cell Pathway Regulation: Cell proliferation; Inhibition; hsa05200
• Cell Pathway Regulation: Mitochondrial apoptotic signaling pathway; Activation; hsa04210
• In Vitro Model: GBM cells; Brain; Homo sapiens (Human); N.A.
• In Vivo Model: Nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blot analysis
• Experiment for Drug Resistance: CCK8 assay; Flow cytometry assay
• Mechanism Description: miR-143 enhances the antitumor activity of shikonin by targeting BAG3 and reducing its expression in human glioblastoma stem cell.

References

• Ref 1: MiR-143 enhances the antitumor activity of shikonin by targeting BAG3 expression in human glioblastoma stem cells. Biochem Biophys Res Commun. 2015 Dec 4-11;468(1-2):105-12. doi: 10.1016/j.bbrc.2015.10.153. Epub 2015 Nov 2.