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Kobe0065

Catalog No. T1876 CAS 436133-68-5

Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.

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Kobe0065, CAS 436133-68-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 57.00
25 mg	In stock	$ 98.00
50 mg	In stock	$ 143.00
100 mg	In stock	$ 233.00
200 mg	In stock	$ 387.00
500 mg	In stock	$ 646.00

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Purity: 99.76%

Purity: 99.58%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
Targets&IC50	C-Raf1 RBD:46 ± 13 μM(ki)
In vitro	Kobe0065-family compounds bind to Ras?GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras?GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition[1].
In vivo	Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1].
Kinase Assay	Determination of lipase activity: For determination of lipase activity, lysates are incubated with a substrate containing radiolabeled [9,10-3H(N)]-triolein. Subsequently, FA are extracted and quantitated by liquid scintilation counting. Data are presented as mean S.D. of triplicate determinations and representative for at least three independent experiments.
Cell Research	NIH 3T3 cells are transfected with pEF-BOS-HA-H-Ras(G12V) or an empty vector and treated with the 2 and 20 μM compound or the vehicle (DMSO) in the presence of 2% FBS for 1 h. Cell lysate is subjected to detection of c-Raf-1 coimmunoprecipitated with an anti-H-Ras antibody and total c-Raf-1 by Western blotting with an anti-c-Raf-1 antibody. Immunoprecipitated H-Ras(G12V) are detected by an anti-HA antibody.(Only for Reference)

Molecular Weight	449.79
Formula	C15H11ClF3N5O4S
CAS No.	436133-68-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 4.5 mg/mL (10 mM)), Heating is recommended.

References and Literature

1. Shima F, et al. Proc Natl Acad Sci U S A. 2013, 110(20):8182-7.

Citations

1. Wang J, Yao N, Hu Y, et al. PHLDA1 promotes glioblastoma cell growth via sustaining the activation state of Ras. Cellular and Molecular Life Sciences. 2022 Sep 15;79(10):520.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Kinase Inhibitor Library Inhibitor Library Bioactive Compound Library Anti-Colorectal Cancer Compound Library Anti-Cancer Metabolism Compound Library Autophagy Compound Library Anti-Ovarian Cancer Compound Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library

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Keywords

Kobe0065 436133-68-5 Apoptosis GPCR/G Protein MAPK Raf Ras inhibit Inhibitor Kobe-0065 Kobe 0065 inhibitor

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