PROTACs
-
PROTACs Related Products (429)
Related Products (429)
-
ARD-2585
0 ImagesARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
-
PROTAC IRAK3 degrade-1 formic
0 ImagesCat. No.: HY-142662APurity: 99.26%
-
DAS-5-oCRBN
0 ImagesDAS-5-oCRBN is a PROTAC molecule with both c‑Src kinase inhibitory activity and target protein degradation activity, with an EC50 of 45 nM for c‑Src binding. DAS-5-oCRBN binds non-covalently to Cereblon and mediates target protein degradation via the ubiquitin-proteasome pathway. DAS-5-oCRBN can catalytically deplete intracellular c‑Src protein, while blocking both the kinase catalytic function of c‑Src and the non-catalytic protein interactions mediated by its SH2 and SH3 domains. DAS-5-oCRBN inhibits tumor cell proliferation and exerts significant anti-proliferative effects on both c‑Src kinase activity-dependent MDA-MB-231 cells and c‑Src protein level-dependent CAL51 cells. DAS-5-oCRBN can be used in cancer-related research such as studies on triple-negative breast cancer and chronic myeloid leukemia.
-
MS6105
0 ImagesMS6105 is a PROTAC degrader targeting LDHA and LDHB, with DC50 values of 38 nM and 74 nM for degrading LDHA and LDHB in PANC-1 cells, respectively, and no hook effect is observed at high concentrations. MS6105 inhibits the proliferation of pancreatic cancer cells, and no obvious toxicity is observed after intraperitoneal administration in mice. MS6105 can be used for pancreatic cancer-related research.
-
ARD-2128
0 ImagesARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
-
PROTAC KDM3 degrader-1
0 ImagesPROTAC KDM3 degrader-1 is a KDM3A/KDM3B PROTAC degrader with DC50 values of 13.73 nM and 172.6 nM in SW480 cells, respectively. PROTAC KDM3 degrader-1 induces cereblon-dependent proteasomal degradation of KDM3A and KDM3B. PROTAC KDM3 degrader-1 inhibits the oncogenic Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 eliminates colorectal cancer stem cells, suppresses their self-renewal, and blocks colony formation of colorectal cancer cells. PROTAC KDM3 degrader-1 inhibits tumor growth in a colorectal cancer xenograft mouse model. PROTAC KDM3 degrader-1 can be used for the research of colorectal cancer.
-
GDC-2992
0 ImagesSynonyms: RO7656594GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study.
-
PROTAC PTPN2 degrader-1
0 ImagesCat. No.: HY-148691CAS No.: 2655638-07-4PROTAC PTPN2 degrader-1 is a PROTAC degrader targeting non-receptor protein tyrosine phosphatase 2 (PTPN2), with a DC50 of 18 nM in 293T cells. It exhibits an IC50 of 22 nM against PTPN2. Through highly selective degradation and inhibition of PTPN2 phosphatase, PROTAC PTPN2 degrader-1 relieves the negative regulation of the IFNγ pathway, upregulates interferon signaling, activates effector T cells, and enhances anti-tumor immunity. PROTAC PTPN2 degrader-1 can be used in melanoma-related research.
-
PROTAC AR Degrader-8
0 ImagesPROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC50s of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 values of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer.
-
dTAG-47-NEG
0 ImagesCat. No.: HY-147099Purity: 98.93%dTAG-47-NEG is an inactive bifunctional negative control PROTAC and also the diastereomer of dTAGV-1 (HY-145514D). dTAG-47-NEG does not reduce the level of BCL11A-FKBP12F36V, nor does it induce the degradation of BCL11A-FKBP12F36V, proteins tagged with FKBP12F36V, wild-type FKBP12, FKBP12F36V-KRASG12V or FKBP12F36V-EWS/FLI. dTAG-47-NEG exerts no antiproliferative effect in cancer cells.
-
ARD-1676
0 ImagesCat. No.: HY-156111CAS No.: 2632305-36-1ARD-1676 is an orally active androgen receptor (AR) PROTAC degrader. ARD-1676 induces proteasomal degradation of AR, inhibits AR-regulated gene expression, suppresses cell growth, reduces AR protein levels and inhibits tumor growth in in vivo models. ARD-1676 can be used in studies related to AR+ human prostate cancer and spinal bulbar muscular atrophy.
-
NRX-0492
0 ImagesNRX-0492 is an orally active BTK PROTAC degrader, with a binding IC50 of 1.2 nM for both wild-type BTK and BTKT474I, and 2.7 nM for BTKC481S, and exhibits cellular DC50 values of 0.1 nM and 0.2 nM against wild-type BTK and BTKC481S, respectively. NRX-0492 catalyzes the ubiquitination and proteasomal degradation of wild-type and drug-resistant mutant BTK by recruiting the CRBN E3 ubiquitin ligase complex. NRX-0492 inhibits the BCR signaling pathway and its downstream NF-κB/MYC transcriptional program, achieves rapid and sustained degradation in primary CLL cells, and exhibits extremely low cytotoxicity. NRX-0492 degrades BTK, inhibits tumor cell proliferation and activation, and significantly suppresses tumor growth in xenograft models. NRX-0492 can be used in research related to chronic lymphocytic leukemia and diffuse large B-cell lymphoma.
-
HLB-0532259
0 ImagesHLB-0532259 is a Aurora-A/N-Myc PROTAC degrader, with a DC50 of 20.2 nM against Aurora-A in MCF-7 cells; its DC50 values against N-Myc are 179 nM in SK-N-BE (2) cells and 229 nM in Kelly cells, respectively. HLB-0532259 induces apoptosis (apoptosis) in MYCN-amplified neuroblastoma cells and inhibits tumor growth in mouse xenograft models. HLB-0532259 can be used for the research of neuroblastoma.
-
R1-ICR-5
0 ImagesR1-ICR-5 is a highly selective RIPK1 PROTAC degrader. Mediated by VHL, R1-ICR-5 induces the degradation of RIPK1, which in turn dysregulates the TNFR1 and TLR3/4 signaling hubs, enhances the signaling outputs of NF-κB, MAPK and IFN, and simultaneously promotes RIPK3 activation and necroptosis (necroptosis). R1-ICR-5 can be used in the research of triple-negative breast cancer and skin inflammation.
