CDK8-IN-13

CAS No. 918523-75-8

CDK8-IN-13( —— )

Catalog No. M36400 CAS No. 918523-75-8

CDK8-IN-13 is a CDK8 inhibitor (IC50: 51.9 nM) with potent, selective and oral activity. CDK8-IN-13 induces apoptosis and reduces the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 exhibits anti-tumour activity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 73 In Stock
5MG 73 In Stock
10MG 93 In Stock
25MG 179 In Stock
50MG 272 In Stock
100MG 403 In Stock
200MG 585 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    CDK8-IN-13
  • Note
    Research use only, not for human use.
  • Brief Description
    CDK8-IN-13 is a CDK8 inhibitor (IC50: 51.9 nM) with potent, selective and oral activity. CDK8-IN-13 induces apoptosis and reduces the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 exhibits anti-tumour activity.
  • Description
    CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces Apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity.
  • In Vitro
    Cell Proliferation AssayCell Line:molm-13, HL-60, MV4-11, MGC-803, MDA-MB-231, A375, A549 cells Concentration:0-50 μM Incubation Time:Result:Showed antiproliferative activity with GC50s of 1.57, 1.00, 4.61, >50, >50, >50, >50 μM, respectively.Western Blot Analysis Cell Line:HCT-116 cells Concentration:1, 2.5, 5, 10 μM Incubation Time:12 h Result:Decreased the expression of p-STAT1 S727 and p-STAT5 S726, andsuppressed the phosphorylation of STAT1 S727 induced by IFN-γ (10 ng/mL) in a dose-dependent manner.Apoptosis Analysis Cell Line:HL-60 cells Concentration:0, 1, 5, 10 μM Incubation Time:48 h Result:Induced approximately 7% and 36% apoptotic at concentrations of 5 and 10 μM, respectively.
  • In Vivo
    Animal Model:6-week-old Balb/C mice (C1498 cells)Dosage:40, 80 mg/kg Administration:P.o.; for 15 days Result:Decreased the tumor growth with no significant weight loss,the expression of Ki67 decreased in a dose-dependent manner, the level of phosphorylation of STAT1 S727 in tumor tissues was downregulated.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    Apoptosis | CDK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    918523-75-8
  • Formula Weight
    237.26
  • Molecular Formula
    C14H11N3O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 125 mg/mL (526.85 mM; Ultrasonic )
  • SMILES
    C(N)(=O)C=1C=C(C=2C=C3C(=NC2)NC=C3)C=CC1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Zhang XX, et al. Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia. Eur J Med Chem. 2023 May 5;251:115214.?
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