Epigenetics

Remodelin HBr salt is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.

Remetinostat is a hydroxamic acid-based inhibitor of histone deacetylase enzymes. It is under development for the treatment of cutaneous T-cell lymphoma.

RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.

RBN012759, a potent and selective PARP14 inhibitor, decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.

R 59949 is used as a Diacylglycerol kinase (DGK) inhibitor.

Quercetagetin (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu. It is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50: 0.34 μM).

QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).

PTACH (NCH-51) is a SAHA-based inhibitor of human HDAC. It can potently inhibit the growth of various human Y cells (EC50: 1 to 10 μM).

PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity. PS315 is a derivative of PS48 and is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing displacement of the active site residue Lys111.

Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) with a Ki of 6 μM. Protein kinase inhibitor H-7 is also a cyclic nucleotide dependent protein kinase inhibitor.

Protein Kinase C 19-31 acetate, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity.

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM).

PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader with IC50 of 13.5 nM.

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

PROTAC BET Degrader-3 is a potent degrader OF BET based on PROTAC.

PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.