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
All Product Categories
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PROTACs Related Products (1334)
Related Products (1334)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC PD-1/PD-L1 degrader-1
0 ImagesPROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
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LD4172
0 ImagesLD4172 is a selective RIPK1 PROTAC degrader with a Ki of 4.8 nM. LD4172 induces RIPK1 protein degradation via ternary complex formation with RIPK1 and VHL E3 ligase, driving ubiquitination and proteasomal breakdown. LD4172 abrogates TNF-induced classical NF-κB signaling in TRAF2-deficient cells, impairing IκBα phosphorylation and degradation, and reducing IL-8 production. LD4172 induces apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy. LD4172 acts as a chemical probe for investigating RIPK1 scaffolding functions. LD4172 can be used for the research of melanoma, colon cancer.
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BSJ-02-162
0 ImagesSynonyms: CDK4/6-IN-11BSJ-02-162 (CDK4/6-IN-11) is a CDK4/CDK6 and IKZF1/IKZF3 degrader, with DC50 values of 32 nM and 6.1 nM against CDK4 and CDK6, respectively; its IC50 ranges from 1 to 50 nM. BSJ-02-162 induces G1-phase cell cycle arrest, reduces phosphorylated retinoblastoma protein levels, and exerts antiproliferative activity in mantle cell lymphoma cells. BSJ-02-162 is applicable to research related to mantle cell lymphoma.
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dBRD 9-A
0 ImagesdBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma.
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TMX-4153
0 ImagesTMX-4153 is a selective PIP4K2C PROTAC degrader. TMX-4153 induces PIP4K2C degradation in MOLT4 cells (DC50 = 24 nM) and HAP1 cells (DC50 = 361 nM). TMX-4153 can be used for the study of biological functions of PIP4K2C (immune modulation)-related diseases. (Pink: BTK ligand (HY-177432), Blue: VHL Ligand (HY-112078), Black: Linker).
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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.
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JPS014 TFA
0 ImagesCat. No.: HY-145815APurity: 98.12%JPS014 TFA is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3, with DC50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 TFA recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS014 TFA acts as a submicromolar inhibitor of the HDAC1-CoREST, HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 TFA increases the level of H3K56ac, reduces the stability of LSD1 and SIN3A, and induces cell apoptosis (apoptosis). JPS014 TFA can be used for the research of colon cancer.
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PARP1 PROTAC 180055
0 ImagesCat. No.: HY-170620Purity: 98.90%PARP1 PROTAC 180055 is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells.
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TMX-2172
0 ImagesTMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC50 values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer.
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SK2187
0 ImagesCat. No.: HY-171768CAS No.: 3038446-91-9Synonyms: JB301SK2187 (JB301) is a selective AURKA PROTAC degrader with a DC50 of about 10 nM. SK2187 exhibits growth inhibition against NGP cells with an IC50 of 101.5 nM. SK2187 can be used for the study of MYCN-amplified neuroblastoma.
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ZLC491
0 ImagesZLC491 is an orally active PROTAC degrader that selectively targets CDK12/CDK13 and exhibits certain oral bioavailability. ZLC491 induces cereblon- and proteasome-dependent selective degradation of CDK12 and CDK13. ZLC491 inhibits the transcription and expression of long genes, and mainly acts on a subset of DNA damage response genes. ZLC491 inhibits the proliferation of various triple-negative breast cancer cells. ZLC491 can be used in research related to triple-negative breast cancer.
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MG-277
0 ImagesMG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.
