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2OH-BNPP1 

Cat. No.: HY-102081 Purity: 99.65%
Handling Instructions

2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.

For research use only. We do not sell to patients.

2OH-BNPP1 Chemical Structure

2OH-BNPP1 Chemical Structure

CAS No. : 833481-73-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 196 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 196 In-stock
Estimated Time of Arrival: December 31
Solid
2 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Estimated Time of Arrival: December 31
10 mg USD 384 In-stock
Estimated Time of Arrival: December 31
25 mg USD 792 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2280 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.

IC50 & Target

BUB1 kinase[1]

In Vitro

2OH-BNPP1 (0.1-50 μM) abrogates TGFβ signaling in a dose dependent manner. 2OH-BNPP1 dose-dependently impairs the TGFβ-induced phosphorylation of proteins that mediate canonical and non-canonical TGFβ signaling in multiple cancer cell lines and normal cell lines[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

2OH-BNPP1 (50 mg/kg) blocks TGFβ signaling in vivo, and significantly decreases abundance of phosphorylated SMAD2 in tumor-bearing mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

297.35

Formula

C₁₆H₁₉N₅O

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (336.30 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3630 mL 16.8152 mL 33.6304 mL
5 mM 0.6726 mL 3.3630 mL 6.7261 mL
10 mM 0.3363 mL 1.6815 mL 3.3630 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

In vitro kinase assays are performed using 200 ng of protein (BUB1-WT, or a kinase inactive mutant BUB1-KD), and 2 µg of substrate (TGFBRI-WT, TGFBRI-KD, SMAD3 or H2A) in 1X kinase buffer (50 mM Tris-HCl, 150 mM NaCl, 10 mM MgCl2, 1% (v/v) Glycerol, 0.1% (v/v) Triton X 100, DTT, PMSF, Na3VO4 (1 mM each), 2 mM NaF and β-glycerol phosphate) in 20 µL volume containing 10 µCi 32p-ATP and 300 µM cold ATP. Reactions are run at 30ºC for 0.5-1 hour and quenched using Laemmli buffer and resolved using a 4-12% Bis-Tris gel. Quantitative autoradiography is performed using a Typhoon FLA 9000 scanner.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Cell line-derived xenografts are established by implanting 2.5×106 A549 cells subcutaneously into each flank of 4-6 week old male SCID mice. When tumors reach a volume between 40 to 60 mm3, mice are injected with a single intraperetoneal dose of SB431542 (10 mg/kg body weight), a dose previously reported to inhibit TGFβ signaling in mouse models, or 2OH-BNPP1 (50 mg/kg), or vehicle (DMSO). Tumors are excised 4 hours after treatment and fixed in formalin. Paraffin-embedded sections are stained using an antibody for phosphorylated SMAD2, and micrographs are taken with an Olympus microscope fitted with an Olympus DP-70 high resolution digital camera. The proportion of nuclei that stains positive for phosphorylated SMAD2 are counted in three random fields per tumor per treatment condition [vehicle (n=4), SB431542 (n=2), and 2OH-BNPP1 (n=5)]. A two -ided Student's t-test is performed to assess statistical significance. Slides are adjusted for brightness and contrast with Adobe Photoshop CS2, but the micrographs undergo no further manipulations.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
2OH-BNPP1
Cat. No.:
HY-102081
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