protac(h pgds) 7

PROTAC(H-PGDS)-7 is a selective and potent small molecule hematopoietic prostaglandin D synthase (H-PGDS) PROTAC degradation agent that exhibits degradation activity in KU812 cells with a DC50 of 17.3 pM. It effectively inhibits prostaglandin D2 (PGD2) and is a candidate compound for the treatment of DMD and other H-PGDS-related diseases.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

Protein kinase inhibitor H-7 (5-(2-methylpiperazine-1-sulfonyl)isoquinoline) 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 inhibitor H-7 dihydrochloride(H-7 dihydrochloride) is a potent protein kinase C (PKC) inhibitor. Protein kinase inhibitor H-7 dihydrochloride (100 μM) significantly inhibits TPA (skin tumor promoter, 12-O-tetradecanoylphorbol-13-acetate) and phospholipase C-induced ODC (ornithine decarboxylase) inhibited PMA-induced promiscuity cell lysis activity.

PROTAC CDK9 degrader-7 is a proteolysis-targeting chimera (PROTAC) engineered to selectively target and mediate the degradation of Cyclin-Dependent Kinase 9 (CDK9) via the proteasome pathway [1].

PROTAC(H-PGDS)-8 is a PROTAC degrader targeting Hematopoietic prostaglandin D synthase (H-PGDS), exhibiting an IC50 of 0.14 μM [1].

PROTAC ERα Degrader-7 (Compound i-320) is a powerful PROTAC degrader targeting the estrogen receptor alpha (ERα), exhibiting a DC50 of 0.000006 µM. This compound consists of a cereblon-binding segment, LBM, connected to ERBM, an ERα-binding ligand that includes a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring [1].

PROTAC BRD9 Degrader-7 is a selective and orally active BRD9 degrader with a DC50 of 1.02 nM and demonstrates superior pharmacokinetics, evidenced by a Cmax of 3436.95 ng/mL [1].

PROTACSMARCA2 degrader-7 (Compound I-428) is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI SNF complex. In MV411, it achieves degradation of SMARCA2 and SMARCA4 with DC50 values of <100 nM and 100-500 nM, respectively.

PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting agent targeting EGFR L858R T790M mutations with a DC50 of 13.2 nM. It effectively inhibits proliferation in NCI-H1975 cells with an IC50 of 46.82 nM and significantly induces apoptosis and G2 M phase arrest in these cells. Demonstrating antitumor efficacy, PROTAC EGFR degrader 7 holds promise for non-small cell lung cancer (NSCLC) research [1].

(2'R,7R,8R,10S,13S,14S)-Methyl 10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate is a useful organic compound for research related to life sciences. The catalog number is T65404 and the CAS number is 95716-70-4.

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective, CRBN-recruiting EGFRL858R T790M degrader with a DC50 of 13.2 nM. It effectively inhibits NCI-H1975 cell proliferation with an IC50 of 46.82 nM, induces apoptosis, and causes G2 M phase arrest. This compound shows antitumor activity and is applicable in non-small cell lung cancer (NSCLC) research.

(1'R,3a'R,8a'S,9'S,9a'S)-1'-Methyl-3'-oxo-N,N-diphenyl-3',3a',5',7',8',8a',9',9a'-octahydro-1'H-spiro[[1,3]dioxolane-2,6'-naphtho[2,3-c]furan]-9'-carboxamide is a useful organic compound for research related to life sciences. The catalog number is T67324 and the CAS number is 900160-98-7.

PROTAC BRD4 Degrader-7, a potent bromodomain BRD4 inhibitor exemplified by compound 1a, demonstrates half-maximal inhibitory concentrations (IC50s) of 15.5 nM and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively [1].

PROTAC IRAK4 degrader-7 (Compound I-417) is an orally administered agent with antitumor properties, functioning as a PROTAC IRAK4 degrader [1].