Cart
sales@molnova.com
PBRM1-BD2-IN-5
CAS No. 2819989-61-0
PBRM1-BD2-IN-5( —— )
Catalog No. M35352 CAS No. 2819989-61-0
PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, with dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5 respectively, and an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 180 | In Stock |
|
| 5MG | 187 | In Stock |
|
| 10MG | 275 | In Stock |
|
| 25MG | 453 | In Stock |
|
| 50MG | 591 | In Stock |
|
| 100MG | 820 | In Stock |
|
| 200MG | 1097 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
-
Product NamePBRM1-BD2-IN-5
-
NoteResearch use only, not for human use.
-
Brief DescriptionPBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, with dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5 respectively, and an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2.
-
DescriptionPBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer.
-
In VitroPBRM1-BD2-IN-5 (compound 16) (0-10 μM; 5 days) inhibits PBRM1-expressed LNCaP cells, and reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides.Cell Viability Assay Cell Line:LNCaP cells expressing lentiviral shPBRM1 Concentration:0, 0.1, 1 and 10 μM Incubation Time:5 days Result:Exhibited a more significant effect on LNCaP viability in cells with native PBRM1 levels than in cells with PBRM1 knockdown.Reduced the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides.
-
In Vivo——
-
Synonyms——
-
PathwayChromatin/Epigenetic
-
TargetEpigenetic Reader Domain
-
RecptorEpigenetic Reader Domain
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number2819989-61-0
-
Formula Weight272.73
-
Molecular FormulaC15H13ClN2O
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 100 mg/mL (366.66 mM; Ultrasonic )
-
SMILESO=C1C=2C(NC(N1)C3=CC(C)=CC=C3)=CC=CC2Cl
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Shishodia S, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13.?
molnova catalog
related products
-
SR-0813
SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9, with an IC50 of 25 nM and EC50 of 205 nM for the ENL YEATS domain, and an IC50 of 311 nM and EC50 of 76 nM (CETSA) for the AF9 YEATS domain.
-
Cyclogalegenol
Astramembrangenin (Cycloastragenol) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus.?Cycloastragenol (CAG) may have a novel therapeutic role in depression.
-
GSK046
GSK046 is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins(IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively).
