PROTAC CDK9 Degrader-1 is a selective CDK9 degrader.
PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6)[1].
E3 ligase Ligand 9 is a Ligand of BETd-260 for E3 Ligase used in PROTAC. BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 51 pM against BRD4 protein in RS4;11 leukemia cell line[1].
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader[1].
PROTAC α-synuclein degrader 5 is a highly selective small-molecule degraders (PROTAC) of α-synuclein aggregates, with an DC50 of 7.51 μM and the highest degradation rate Dmax of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research[1].
SNX7886 is a potent protac degrader of CDK8/19. SNX7886 degrades CDK 8 and CDK 19 with 90% and 80% degradation in 293 cells, respectively[1].
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells[1].
PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, with a DC50 of 49 nM[1].
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1].
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37 nM for binding affinity to ALK[1].
MS98 is a potent and selective PROTAC AKT degrader. MS98 depletes cellular total AKT (T-AKT) with the DC50 value of 78 nM. MS98 binds to AKT1, AKT2, and AKT3 with Kds of 4 nM, 140 nM, and 8.1 nM, respectively[1].
GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth[1].
FC-11 is a PROTAC FAK degrader (DC90: 1 nM) . FC-11 contains CRBN ligand Pomalidomide (HY-10984), linker and FAK ligand PF562271 (HY-10459). FC-11 degrades FAK in various cells, with DC50s of 310 pM in TM3, 80 pM in PA1, 330 pM in MDA-MB-436, 370 pM in LNCaP, and 40 pM in Ramos cells[1].
CD147 degrader 1 is a PROTAC targets CD147 with an DC50 value of 6.72 µM. CD147 degrader 1 inhibits cell proliferation, migration and invasion. CD147 degrader 1 decreases the expression of CD147, MMP9, and p-STAT3 protein. CD147 degrader 1 shows anti-cancer acyivity[1].
SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM[1].
CMP98, a PROTAC, is unable to induce degradation of VHL. CMP98 can be used as a negative control compound for CM11[1].
A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP)[1].
JH-XI-10-02 is a potent and selective degrader of CDK8, with an IC50 of 159 nM, based on PROTAC. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19[1].
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1].
PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC50 of 0.03 μM in HT1080 cells[1].
KRAS G12D inhibitor 17 (example 8) is a quinazoline-linked (4R)-4-hydroxy-L-prolinamide compound, inducing degradation of G12D-mutation KRAS protein[1].
PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS[1].
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].
BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research[1].
PROTAC K-Ras Degrader-1 (Compound 518) is potent K-Ras degrader based PROTAC, exhibits ≥70% degradation efficacy in SW1573 cells[1].
QCA570 is a potent BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein.
XZ739, a CRBN-dependent PROTAC BCL-XL degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis[1].
PEG6-(CH2CO2H)2 is a symmetric PEG PROTAC linker, for the synthesis of Homo-PROTACs which is bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation[1].
Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3[1].