WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H558212
CAS#: 329710-24-9
Description: KP372-1 is a synthetic small molecule AKT inhibitor. KP372-1 is consisted of two isomers: KP372-1 A and KP372-1B. KP372-1 showed activities to block signalling downstream of Akt in thyroid tumour cells, leading to inhibition of cell proliferation and increased apoptosis. KP372-1 has also been shown to suppress cell proliferation and induce apoptosis in gliobastoma.
Hodoodo Cat#: H558212
Name: KP372-1
CAS#: 329710-24-9
Chemical Formula: C10H4N6O
Exact Mass: 224.04
Molecular Weight: 224.178
Elemental Analysis: C, 53.58; H, 1.80; N, 37.49; O, 7.14
Synonym: KP3721, KP 3721, KP-3721
IUPAC/Chemical Name: KP372-1A: 10H-indeno[2,1-e]tetrazolo[1,5-b][1,2,4]triazin-10-one
InChi Key: SSNMLKNJEUSPDY-UHFFFAOYSA-N
InChi Code: InChI=1S/C10H4N6O/c17-9-6-4-2-1-3-5(6)7-8(9)11-10-12-14-15-16(10)13-7/h1-4H
SMILES Code: O=C(C1=NC2=NN=NN2N=C13)C4=C3C=CC=C4
Appearance: Solid powder
Purity: >98%
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 224.18 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Liu B, Wu JM, Li J, Liu JJ, Li WW, Li CY, Xu HL, Bao JK. Polygonatum cyrtonema lectin induces murine fibrosarcoma L929 cell apoptosis and autophagy via blocking Ras-Raf and PI3K-Akt signaling pathways. Biochimie. 2010 Dec;92(12):1934-8. Epub 2010 Aug 14. PubMed PMID: 20713122.
2: Shao H, Yi XM, Wells A. Epidermal growth factor protects fibroblasts from apoptosis via PI3 kinase and Rac signaling pathways. Wound Repair Regen. 2008 Jul-Aug;16(4):551-8. PubMed PMID: 18638274; PubMed Central PMCID: PMC2547354.
3: Xi RG, Huang J, Li D, Wang XB, Wu LJ. Roles of PI3-K/Akt pathways in nanoparticle realgar powders-induced apoptosis in U937 cells. Acta Pharmacol Sin. 2008 Mar;29(3):355-63. PubMed PMID: 18298901.
4: Li D, Cui Q, Chen SG, Wu LJ, Tashiro S, Onodera S, Ikejima T. Inactivation of ras and changes of mitochondrial membrane potential contribute to oridonin-induced autophagy in a431 cells. J Pharmacol Sci. 2007 Sep;105(1):22-33. PubMed PMID: 17895587.
5: Zeng Z, Samudio IJ, Zhang W, Estrov Z, Pelicano H, Harris D, Frolova O, Hail N Jr, Chen W, Kornblau SM, Huang P, Lu Y, Mills GB, Andreeff M, Konopleva M. Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia. Cancer Res. 2006 Apr 1;66(7):3737-46. PubMed PMID: 16585200.
6: Koul D, Shen R, Bergh S, Sheng X, Shishodia S, Lafortune TA, Lu Y, de Groot JF, Mills GB, Yung WK. Inhibition of Akt survival pathway by a small-molecule inhibitor in human glioblastoma. Mol Cancer Ther. 2006 Mar;5(3):637-44. PubMed PMID: 16546978.
7: Mandal M, Younes M, Swan EA, Jasser SA, Doan D, Yigitbasi O, McMurphey A, Ludwick J, El-Naggar AK, Bucana C, Mills GB, Myers JN. The Akt inhibitor KP372-1 inhibits proliferation and induces apoptosis and anoikis in squamous cell carcinoma of the head and neck. Oral Oncol. 2006 Apr;42(4):430-9. Epub 2006 Jan 27. PubMed PMID: 16442835; PubMed Central PMCID: PMC1414640.
8: Mandal M, Kim S, Younes MN, Jasser SA, El-Naggar AK, Mills GB, Myers JN. The Akt inhibitor KP372-1 suppresses Akt activity and cell proliferation and induces apoptosis in thyroid cancer cells. Br J Cancer. 2005 May 23;92(10):1899-905. PubMed PMID: 15870708; PubMed Central PMCID: PMC2361761.
