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GK921

Cat. No. M9215
GK921 Structure
Size Price Availability Quantity
2mg USD 290 In stock
5mg USD 430 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

GK921 showed cytotoxicity to RCC (average GI50 in eight RCC cell lines: 0.905 μM). A single treatment with GK921 almost completely reduced tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models. GK921 rescues p53 levels and consequently induces apoptosis; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 344.41
Formula C21H20N4O
CAS Number 1025015-40-0
Purity >98%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

Discovery of a novel target for renal cell carcinoma: transglutaminase 2.
Kang JH, et al. Cell Death Dis. 2016 Apr 21;7:e2200. PMID: 27100894.

Renal cell carcinoma escapes death by p53 depletion through transglutaminase 2-chaperoned autophagy.
Kang JH, et al. Cell Death Dis. 2016 Mar 31;7:e2163. PMID: 27031960.

Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models.
Ku BM, et al. J Cancer Res Clin Oncol. 2014 May;140(5):757-67. PMID: 24610445.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GK921 supplier, inhibitors

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