2. Epigenetics
  3. Epigenetic Reader Domain
  4. PBRM1-BD2-IN-2

PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer.

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

PBRM1-BD2-IN-2 Chemical Structure

PBRM1-BD2-IN-2 Chemical Structure

CAS No. : 2819989-57-4

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Based on 1 publication(s) in Google Scholar

PBRM1-BD2-IN-2 Related Antibodies

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Description

PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer[1].

IC50 & Target

Kd: 9.3 μM (PBRM1-BD2), 10.1 μM (PBRM1-BD5), 18.4 μM (SMARCA2B), 69 μM (SMARCA4)[1].
IC50: 1.0 μM (PBRM1-BD2)[1].
In Vitro

PBRM1-BD2-IN-2 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line[1].
PBRM1-BD2-IN-2 has binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B amd SMARCA4 with Kd values of 9.3 μM, 10.1 μM, 18.4 μM and 69 μM, respectively[1].
PBRM1-BD2-IN-2 has inhibitory activity for PBRM1-BD2 with IC50 value of 1.0 μM[1].

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

PBRM1-BD2-IN-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human prostate cell lines LNCaP, PC3, and RWPE-1
Concentration: 0, 0.1, 1, and 10 μM
Incubation Time: 5 days
Result: Inhibited LNCaP growth at higher concentrations.
Molecular Weight

311.14

Formula

C14H9Cl2FN2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(C2=C(F)C=CC=C2Cl)NC3=C1C(Cl)=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 45 mg/mL (144.63 mM; Need ultrasonic and warming; 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 3.2140 mL 16.0699 mL 32.1399 mL
5 mM 0.6428 mL 3.2140 mL 6.4280 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. 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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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
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. 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 3.2140 mL 16.0699 mL 32.1399 mL 80.3497 mL
5 mM 0.6428 mL 3.2140 mL 6.4280 mL 16.0699 mL
10 mM 0.3214 mL 1.6070 mL 3.2140 mL 8.0350 mL
15 mM 0.2143 mL 1.0713 mL 2.1427 mL 5.3566 mL
20 mM 0.1607 mL 0.8035 mL 1.6070 mL 4.0175 mL
25 mM 0.1286 mL 0.6428 mL 1.2856 mL 3.2140 mL
30 mM 0.1071 mL 0.5357 mL 1.0713 mL 2.6783 mL
40 mM 0.0803 mL 0.4017 mL 0.8035 mL 2.0087 mL
50 mM 0.0643 mL 0.3214 mL 0.6428 mL 1.6070 mL
60 mM 0.0536 mL 0.2678 mL 0.5357 mL 1.3392 mL
80 mM 0.0402 mL 0.2009 mL 0.4017 mL 1.0044 mL
100 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8035 mL
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PBRM1-BD2-IN-2 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:

PBRM1-BD2-IN-22819989-57-4Epigenetic Reader Domainpolybromo-1 (PBRM1)bromodomainbinding affinityinhibitorycancerInhibitorinhibitorinhibit

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