2241237-51-2
2241237-51-2
Chemical Structure
SRX3177
- CAS. Nr.: 2241237-51-2
- Formula:C31H32N6O4S
- Molecular Weight:584.69
InChIKey: XJKTXWSMMWPNTP-UHFFFAOYSA-N
SMILES: O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC=C(NC5=NC6=C(C=C(N6C7CCCC7)C(N(C)C)=O)C=N5)C=C4
Biological Activity: SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer[1][2].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
SRX3177 | 99.33% | SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
CDK9-IN-8 (Standard) | ≥98% | CDK9-IN-8 (Standard) is the analytical standard of CDK9-IN-8 (HY-102039). This product is intended for research and analytical applications. CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC50 of 12 nM. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
SRX3207 | 98.36% | SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Ribociclib | 99.94% | RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Ribociclib hydrochloride (Standard) | 99.96% | Ribociclib (Standard) (LEE011(Standard)) hydrochloride is the analytical standard of Ribociclib hydrochloride (HY-15777A). This product is intended for research and analytical applications. Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
CDK4 degrader 1 | 99.83% | CDK4 degrader 1 is a selective CDK4 molecular glue degrader. CDK4 degrader 1 induces intracellular CDK4 degradation, and its activity is dependent on DCAF16. CDK4 degrader 1 targets the cysteine residue on DCAF16 through its vinylsulfonylpiperazine domain, thereby mediating the degradation of CDK4. CDK4 degrader 1 can be used in research related to cervical cancer. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Aurora-A ligand 1 | 98.75% | Aurora-A ligand 1 is a high-affinity and specific Aurora-A inhibitor with a dissociation constant (Kd) value of 0.85 nM. Aurora-A ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC Aurora-A degraders with antitumor activity. Aurora-A ligand 1 can be used for the synthesis of HLB-0532259 (HY-168439). HLB-0532259 shows anti-tumor activity against neuroblastoma. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
KWZY-11 | KWZY-11 (Compound 11) is a potent PARP/CDK6 dual inhibitor with IC50 values of 156.8, 197.3, and 13.3 nM for PARP1, PARP2, and CDK6, respectively. KWZY-11 inhibits tumor cell proliferation by regulating the Wnt/β-catenin signaling pathway. KWZY-11 induces excessive DNA damage and apoptosis in MDA-MB-231 breast cancer cells. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
LCI133 | LCI133 is afirst-in-class,nanomolar-potent, selective multikinase inhibitor targeting CDK4/6/9 and AURKA/B (IC50 = 4.7/10.2/4.1 nM and 2.8/10.6 nM). LCI133 induces S/G2 cell-cycle arrest and robust apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. LCI133 demonstrates significant antitumor efficacy in a BE(2)-C neuroblastoma xenograft model. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
CDK9 ligand 4 | CDK9 ligand 4 is a CDK9 ligand. As a ligand for target protein for PROTAC (Ligands for Target Protein for PROTAC), CDK9 ligand 4 serves for the development and design of PROTAC CDK9 degraders, such as PROTAC CDK9 degrader-12 (HY-181231). CDK9 ligand 4 is applicable to the research of HIV-1 infection. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Ribociclib impurity 2 | Ribociclib impurity 2 (Ribociclib impurity B) is an impurity of Ribociclib. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Pandey K, et al. SRX3177, a CDK4/6-PI3K-BET inhibitor, in combination with an RdRp inhibitor, Molnupiravir, or an entry inhibitor MU-UNMC-2, has potent antiviral activity against the Omicron variant of SARS-CoV-2. Antiviral Res. 2024 Jul;227:105904. [Content Brief]
- [2]. Burgoyne AM, et al. A triple action CDK4/6-PI3K-BET inhibitor with augmented cancer cell cytotoxicity. Cell Discov. 2020 Jul 28;6(1):49. [Content Brief]
