Company Name: |
TargetMol Chemicals Inc.
|
Tel: |
4008200310 |
Email: |
marketing@tsbiochem.com |
Products Intro: |
Product Name:SETDB1-TTD-IN-1;SETDB1TTDIN1,SETDB1 TTD IN 1,SETDB-1-TTD-IN-1 CAS:2755823-12-0 Purity:99.05% Package:1 mg;10 mg;100 mg;2 mg;25 mg;5 mg
|
|
| 4H-Pyrrolo[3,2-d]pyrimidin-4-one, 3,5-dihydro-2-[[(3R,5R)-1-methyl-5-[4-(phenylmethoxy)phenyl]-3-piperidinyl]amino]-3-(2-propen-1-yl)- Basic information |
Product Name: | 4H-Pyrrolo[3,2-d]pyrimidin-4-one, 3,5-dihydro-2-[[(3R,5R)-1-methyl-5-[4-(phenylmethoxy)phenyl]-3-piperidinyl]amino]-3-(2-propen-1-yl)- | Synonyms: | 4H-Pyrrolo[3,2-d]pyrimidin-4-one, 3,5-dihydro-2-[[(3R,5R)-1-methyl-5-[4-(phenylmethoxy)phenyl]-3-piperidinyl]amino]-3-(2-propen-1-yl)-;SETDB1-TTD-IN-1;SETDB1TTDIN1,SETDB1 TTD IN 1,SETDB-1-TTD-IN-1 | CAS: | 2755823-12-0 | MF: | C28H31N5O2 | MW: | 469.58 | EINECS: | | Product Categories: | | Mol File: | 2755823-12-0.mol | |
| 4H-Pyrrolo[3,2-d]pyrimidin-4-one, 3,5-dihydro-2-[[(3R,5R)-1-methyl-5-[4-(phenylmethoxy)phenyl]-3-piperidinyl]amino]-3-(2-propen-1-yl)- Chemical Properties |
Boiling point | 664.2±65.0 °C(Predicted) | density | 1.24±0.1 g/cm3(Predicted) | storage temp. | 4°C, protect from light, stored under nitrogen | solubility | DMSO : 125 mg/mL (266.20 mM; Need ultrasonic) | pka | 14.81±0.20(Predicted) | form | Solid | color | White to off-white |
| 4H-Pyrrolo[3,2-d]pyrimidin-4-one, 3,5-dihydro-2-[[(3R,5R)-1-methyl-5-[4-(phenylmethoxy)phenyl]-3-piperidinyl]amino]-3-(2-propen-1-yl)- Usage And Synthesis |
Biological Activity | SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a Kd of 88 nM. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD[1].
SETDB1-TTD-IN-1 shows some activity for 53BP1 and JMJD2A, with Kds of 4.3 μM and 86 μM, respectively. SETDB1-TTD-IN-1 does not show activity against 14 of the 16 tested tudor domains (Kd>100 μM)[1].SETDB1-TTD-IN-1 (2.5-40 μM) efficiently and dose-dependently stabilizes the SETDB1-TTD protein in HEK293T cells[1].SETDB1-TTD-IN-1 (2.5-40 μM; 24 h) significantly affected the expression of 72 genes in human acute monocytic leukemia THP-1 cells[1]. | References | [1]. Guo Y, et, al. Structure-Guided Discovery of a Potent and Selective Cell-Active Inhibitor of SETDB1 Tudor Domain. Angew Chem Int Ed Engl. 2021 Apr 12;60(16):8760-8765. |
| 4H-Pyrrolo[3,2-d]pyrimidin-4-one, 3,5-dihydro-2-[[(3R,5R)-1-methyl-5-[4-(phenylmethoxy)phenyl]-3-piperidinyl]amino]-3-(2-propen-1-yl)- Preparation Products And Raw materials |
|