Catalog |
name |
Description |
price |
R-R-2427 |
SRX3177 CAS No.2241237-51-2 |
SRX3177/CAS No.2241237-51-2 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells. |
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R-R-2428 |
SMD-3040 |
SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models. |
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R-R-2429 |
Inobrodib CAS No.2222941-37-7 |
Inobrodib (CCS1477)/CAS No.2222941-37-7 is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression. |
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R-R-2430 |
BRM/BRG1 ATP Inhibitor-1 CAS No.2270879-17-7 |
BRM/BRG1 ATP Inhibitor-1 (compound 14)/CAS No.2270879-17-7 is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity. |
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R-R-2431 |
dBET6 CAS No.1950634-92-0 |
dBET6/CAS No.1950634-92-0 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity. |
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R-R-2432 |
MZ 1 CAS No.1797406-69-9 |
MZ 1/CAS No.1797406-69-9 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively. |
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R-R-2433 |
ARV-825 CAS No.1818885-28-7 |
ARV-825/CAS No.1818885-28-7 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively. |
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R-R-2434 |
666-15 CAS No.1433286-70-4 |
666-15/CAS No.1433286-70-4 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model. |
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R-R-2435 |
SGC-CBP30 CAS No.1613695-14-9 |
SGC-CBP30/CAS No.1613695-14-9 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects. |
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R-R-2436 |
AU-15330 CAS No.2380274-50-8 |
AU-15330/CAS No.2380274-50-8 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity. |
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