PROTACs
PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.
PROTACs Isoform Specific Products
-
PROTACs Related Products (1377)
Related Products (1377)
-
Antibodies (1)
-
PROTACs Isoform Comparison
-
PROTAC BTK Degrader-6
0 ImagesPROTAC BTK Degrader-6 is an orally active PROTAC-based BTK degrader with a DC50 of 3.18 nM. PROTAC BTK Degrader-6 induces BTK degradation via proteasomal degradation, ubiquitination, and CRBN ligase recruitment pathways. PROTAC BTK Degrader-6 inhibits NF-κB activation, mRNA expression of IL-1β and IL-6, as well as the secretion of pro-inflammatory cytokines. PROTAC BTK Degrader-6 reduces inflammatory responses in a zymosan-induced mouse model of peritonitis. PROTAC BTK Degrader-6 can be used in peritonitis-related research.
-
MS4322 (isomer)
0 ImagesSynonyms: YS43-22 (isomer)MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer.
-
PROTAC CDK9 degrader-2
0 ImagesPROTAC CDK9 degrader-2 is a PROTAC degrader targeting CDK9, with an IC50 of 523 nM. PROTAC CDK9 degrader-2 selectively degrades CDK9 via the cereblon-dependent ubiquitin-proteasome pathway and inhibits the proliferation of cancer cells overexpressing CDK9. PROTAC CDK9 degrader-2 can be used for cancer research.
-
UBX-382
0 ImagesCat. No.: HY-160142CAS No.: 2884554-45-2UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers.
-
PD-M6
0 ImagesPD-M6 is a mTOR PROTAC degrader (DC50: 4.8 μM). PD-M6 promotes ubiquitination and degradation of mTOR. PD-M6 downregulates MAPKAP1 and CASTOR1, and induces Autophagy. PD-M6 inhibits the proliferation of cervical cancer, breast cancer and liver cancer cell lines. PD-M6 can be used for the research of cervical cancer, breast cancer and liver cancer.
-
PROTAC IRAK4 degrader-13
0 ImagesPROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC50s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research. Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker
-
Abd110
0 ImagesAbd110 is a selective ATR PROTAC degrader. Abd110 recruits Cereblon to induce the proteasomal degradation of ATR, and reduces the levels of phosphorylated ATR and downstream phosphorylated CHK1. Abd110 can be used for research on pancreatic cancer and cervical cancer.
-
PROTAC PI3Kα degrader-1
0 ImagesCat. No.: HY-174461Purity: 99.21%PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader that recruits CRBN, with a DC50 of 0.08 μM in T47D breast cancer cells. PROTAC PI3Kα degrader-1 inhibits the phosphorylation of AKT at the Ser473 site in cancer cells and exhibits in vivo anticancer efficacy in xenograft models. PROTAC PI3Kα degrader-1 can be used in cancer-related research.
-
SJ1008030 formic
0 ImagesCat. No.: HY-147330BPurity: 98.91%
-
PROTAC c-Met degrader-1
0 ImagesPROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC50 of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer.
-
GP262
0 ImagesGP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110α and p110γ with a DC50 of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) .
-
ACBI-4
0 ImagesCat. No.: HY-176792CAS No.: 3097985-19-5ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with Kd values of 141 nM against KRASG12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer.
-
PSP-0119
0 ImagesPSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC50 = 2.83 nM). PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML).
-
PROTAC NSD3 degrader-1
0 ImagesPROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
-
PROTAC HER2 degrader-1
0 ImagesPROTAC HER2 degrader-1 is a selective HER2 PROTAC degrader with a DC50 of 69 nM. PROTAC HER2 degrader-1 induces ubiquitination and degradation of HER2 via the ubiquitin-proteasome system, thereby inhibiting the downstream PI3K/AKT/mTOR and RAS/RAF/MEK/ERK signaling pathways. PROTAC HER2 degrader-1 inhibits the proliferation of HER2-positive cancer cells, induces apoptosis and arrests the cell cycle. PROTAC HER2 degrader-1 suppresses the growth of HER2-positive xenografts. PROTAC HER2 degrader-1 can be used in HER2-positive cancer-related research.
-
NU223612
0 ImagesNU223612 is a cereblon (CRBN)-recruiting IDO1 PROTAC degrader, with a DC50 value of 0.329-0.5438 μM against human IDO1, and it is capable of penetrating the blood-brain barrier. NU223612 directly binds to IDO1, mediates the degradation of both wild-type and catalytically inactive mutant IDO1 proteins, and does not degrade TDO2. NU223612 inhibits IDO1-mediated enzymatic activity. NU223612 directly binds to CRBN and promotes the formation of a cooperative ternary complex with IDO1. NU223612 induces ubiquitin-dependent proteasomal degradation of the IDO1 protein. NU223612 suppresses IDO1-mediated non-enzymatic phosphorylation of NF-κB p65 and the DNA-binding activity of downstream transcription factors. NU223612 can be used in studies of glioblastoma (malignant glioma).
-
FIP22
0 ImagesFIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis.
