Epigenetic Reader Domain Inhibitor

GSK6853 (Standard) is the analytical standard of GSK6853 (HY-100220). This product is intended for research and analytical applications. GSK6853, a chemical probe, is a potent and selective inhibitor of the BRPF1 bromodomain. GSK6853 shows excellent BRPF1 potency (pKd = 9.5) and greater than 1600-fold selectivity over all other bromodomains.

CBP/p300-IN-24 is a selective CBP bromodomain inhibitor with an IC₅₀ of 32 μM, showing selectivity over BRD4 BD-1 bromodomain. CBP/p300-IN-24 binds to the acetyl lysine binding pocket, forms hydrogen bonds with Asn1168 and a solvent-mediated hydrogen bond with Tyr1125, and forms hydrophobic interactions with Leu1120, Ile1122, and Val1174.

C646 (Standard) is the analytical standard of C646 (HY-13823). This product is intended for research and analytical applications. C646 is a selective and competitive histone acetyltransferase p300 inhibitor with K_i of 400 nM, and is less potent for other acetyltransferases.

TPOP146 (Standard) is the analytical standard of TPOP146 (HY-100697). This product is intended for research and analytical applications. TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.

5-Ph-IAA (Standard) is the analytical standard of 5-Ph-IAA (HY-134653). This product is intended for research and analytical applications. 5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression.

TP-472 (Standard) is the analytical standard of TP-472 (HY-100517). This product is intended for research and analytical applications. TP-472, a chemical probe, is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells.

BAY-299 (Standard) is the analytical standard of BAY-299 (HY-107424). This product is intended for research and analytical applications. BAY-299, a chemical probe, is a very potent, dual inhibitor with IC₅₀s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.

Ertabresib (Standard) (INCB-057643 (Standard)) is the analytical standard of Ertabresib (HY-111485). This product is intended for research and analytical applications. Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer.

Y06137 (Standard) is the analytical standard of Y06137 (HY-111503). This product is intended for research and analytical applications. Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a K_d of 81 nM.

BI-9564 (Standard) is the analytical standard of BI-9564 (HY-100352). This product is intended for research and analytical applications. BI-9564, a chemical probe, is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family.