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BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM.

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

BAP1-IN-1 Chemical Structure

BAP1-IN-1 Chemical Structure

CAS No. : 353495-21-3

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

BAP1-IN-1 Related Antibodies

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Description

BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM[1].

IC50 & Target

IC50: 0.1-1 μM (BAP1)[1]
In Vitro

BAP1-IN-1 (Compound 8) (1 μM; 30 min) specifically inhibits BAP1 not just in vitro but also within the cellular context[1].
BAP1-IN-1 (0.1 μM; 24 h) significantly alters 240 genes in BAP1-WT cells, whereas only 33 transcripts are changed in BAP1-KO cells, demonstrating that the gene expression changes mainly depend on the presence of BAP1 protein[1].
BAP1-IN-1 (0-10 μM; 72 h) selectively inhibits cells with ASXL1 GOF mutations[1].

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

BAP1-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: CAL51 cells
Concentration: 1 μM
Incubation Time: 30 min
Result: Remarkably inhibited BAP1 catalytic activity.

Cell Viability Assay[1]

Cell Line: THP1, MOML13, K562, THP1-ASXL1-WT and THP1-ASXL1-Y591fs cells
Concentration: 0, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 72 h
Result: K562 cells (ASXL1-Y591*) were significantly more sensitive to the treatment. Cells with ASXL1fs mutations were ten times more sensitive to the treatment.
In Vivo

BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice[1].

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

Animal Model: NSGS mice, K562 (ASXL1-WT/Y591*) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588*) model[1]
Dosage: 50 mg/kg/d
Administration: Intraperitoneal injection, drug treatments were started at day 28 after transplantation
Result: Significantly delayed progression of disease in both models.
Molecular Weight

292.33

Formula

C18H16N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=[N+](C1=CC2=C(NC(C3=CC=CC=C3)C4C2C=CC4)C=C1)[O-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (171.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4208 mL 17.1040 mL 34.2079 mL
5 mM 0.6842 mL 3.4208 mL 6.8416 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.52%

COA (250 KB) HNMR (252 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4208 mL 17.1040 mL 34.2079 mL 85.5198 mL
5 mM 0.6842 mL 3.4208 mL 6.8416 mL 17.1040 mL
10 mM 0.3421 mL 1.7104 mL 3.4208 mL 8.5520 mL
15 mM 0.2281 mL 1.1403 mL 2.2805 mL 5.7013 mL
20 mM 0.1710 mL 0.8552 mL 1.7104 mL 4.2760 mL
25 mM 0.1368 mL 0.6842 mL 1.3683 mL 3.4208 mL
30 mM 0.1140 mL 0.5701 mL 1.1403 mL 2.8507 mL
40 mM 0.0855 mL 0.4276 mL 0.8552 mL 2.1380 mL
50 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7104 mL
60 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4253 mL
80 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0690 mL
100 mM 0.0342 mL 0.1710 mL 0.3421 mL 0.8552 mL
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BAP1-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAP1-IN-1353495-21-3OthersBAP1ASXL1K562THP1MOML13Inhibitorinhibitorinhibit

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