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PROTACs

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Cat. No. Product Name Field of Application Chemical Structure
DC78571 UR241-2
UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia.
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DC78570 E3 Ligase Ligand-linker Conjugate 188
E3 Ligase Ligand-linker Conjugate 188 is a E3 ligase ligand-linker conjugate, used for the synthesis of AZ'3137.
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DC78569 PSP-0119
PSP-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).
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DC78559 3-(7-Methoxy-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione-azacyclohexane-C-piperazine-CO
3-(7-Methoxy-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione-azacyclohexane-C-piperazine-CO is a synthesized E3 ligase ligand-linker conjugate that can be used to synthesize PROTAC LRRK2 Degrader-4. PROTAC LRRK2 Degrader-4 is a potent LRRK2 PROTAC degrader with anti-neuroinflammatory activity.
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DC78553 AR-DBD ligand-1
AR-DBD ligand-1 is an AR-DBD ligand. AR-DBD ligand-1 can be used to synthesize PROTAC LYA914.
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DC78540 Azacyclohexane-C-piperazine-C(OCH3)2
Azacyclohexane-C-piperazine-C(OCH3)2 is a PROTAC linker that can be used to synthesize PROTAC LRRK2 Degrader-4. PROTAC LRRK2 Degrader-4 is a potent LRRK2 PROTAC degrader with anti-neuroinflammatory activity.
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DC78539 Azacyclohexane-O-cyclohexane-C-(OCH3)2
Azacyclohexane-O-cyclohexane-C-(OCH3)2 is a PROTAC linker that can be used to synthesize PROTAC LRRK2 Degrader-3. PROTAC LRRK2 Degrader-3 is a potent LRRK2 PROTAC degrader with anti-neuroinflammatory activity.
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DC78529 TH10184
TH10184 is a NUDT5 inhibitor. TH10184 can be conjugated with VH032 and linker to synthesize PROTAC NUDT5 degrader DDD2
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DC78513 BCL6 ligand-5
BCL6 ligand-5 (Compound 37) is a BCL6 ligand. BCL6 ligand-5 can be used as a ligand for target protein for PROTAC to develop and design degraders for PROTAC BCL6, such as PROTAC BCL6 Degrader-2. BCL6 ligand-5 can also be used in tumor research.
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DC78503 BTK/IKZF1/3 ligand 1
BTK/IKZF1/3 ligand 1 is a BTK/IKZF1/3 PROTAC ligand. BTK/IKZF1/3 ligand 1 can be conjugated with E3 ligase Ligand and linker to synthesize PROTAC BTK/IKZF1/3 Degrader-1. PROTAC BTK/IKZF1/3 Degrader-1 can be used for cancer research.
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DC78501 Multi kinase ligand 4
Multi kinase ligand 4 is a target protein ligand used in the synthesis of PROTAC DB-0646.
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DC78499 Dione-piperidine-indazol-piperazin-cyclohexyl-NH2
Dione-piperidine-indazol-piperazin-cyclohexyl-NH2 is an E3 ligase ligand-linker conjugate that incorporates a CRBN ligand and linker. Dione-piperidine-indazol-piperazin-cyclohexyl-NH2 can be used for synthesis of PROTAC MD-4251.
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DC78498 6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole
6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole is an E3 ligase ligand used in the synthesis of the PROTAC Androgen receptor degrader-1.
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DC78491 E3 Ligase Ligand-linker Conjugate 195
E3 Ligase Ligand-linker Conjugate 195 is a conjugate of the CRBN ligand and the linker. E3 Ligase Ligand-linker Conjugate 195 can be used for synthesis of PROTACs such as APH02174.
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DC78487 XB2M54
XB2M54 is a selective XIAP antagonist. XB2M54 inhibits NOD2-mediated inflammatory signaling. XB2M54 is an E3 ligase ligand. XB2M54 can be used for synthesis of PROTAC ERα Degrader-1.
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DC78479 3,9-Dimethyl-3,9-diazaspiro[5.5]undecane
3,9-Dimethyl-3,9-diazaspiro[5.5]undecane is a rigid PROTAC linker can be used in the synthesis of PROTACs, such as FIP22. FIP22 is a potent and selective IRAK4 PROTAC degrader with anti- atopic dermatitis activity.
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DC78464 HPK1 ligand 6
HPK1 ligand 6 is a HPK1 ligand. HPK1 ligand 6 can be used to synthesize PROTAC HPK1 Degrader-6.
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DC78437 FTO ligand-1
FTO ligand-1 is a FTO ligand for FTO PROTAC degrader FP54. FTO ligand-1 can inhibit cell proliferation and block the FP54-induced FTO degradation. FTO ligand-1 can be used for research of cancer, such as acute myeloid leukemia (AML).
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DC78421 STING ligand-4
STING ligand-4 (Compound 2) is a nitro-free covalent STING inhibitor with an IC50 < 0.2 μM. STING ligand-4 can be used for synthesis of PROTAC STING degrader-4.
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DC78410 di-Ellipticine-RIBOTAC TFA
Di-Ellipticine-RIBOTAC TFA (Compound 7) is a RNA RIBOTAC degrader, capable of specifically binding and degrading r(G4C2)exp. Di-Ellipticine-RIBOTAC TFA only cuts the expanded GGGGCC repeat RNA in the pathogenic factor of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) - the chromosome 9 open reading frame 72 (9orf72) gene (r(G4C2)exp), and has no effect on normal short repetitive sequences. Di-Ellipticine-RIBOTAC TFA significantly improves the pathological phenotype of c9ALS/FTD in cells and mouse models. Di-Ellipticine-RIBOTAC TFA can be used for the study of c9ALS/FTD.
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DC78383 Thalidomide-NH-C4
Thalidomide-NH-C4 is an E3 ligase ligand-linker conjugate containing a CRBN ligand and a linker. Thalidomide-NH-C4 can bind to a target protein ligand to form a PROTAC molecule, LD-110.
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DC78357 KI-ARv-03
KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32.
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DC78344 RET ligand-5
RET ligand-5 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC RET Degrader 1. PROTAC RET Degrader 1 is a potent RET PROTAC degrader with anti-tumor activity.
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DC78342 Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine
Thalidomide-OCH2-amide-PEG2-C2-Boc is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-OCH2-amide-PEG2-C2-Boc can be used to synthesize PROTAC CDK4/6/9 degrader 2.
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DC78314 BRD2 BD1 ligand-1
BRD2 BD1 ligand-1 is a potent BRD2 BD1 ligand (Ligands for Target Protein for PROTACs) can be used in the synthesis of PROTAC BRD2 BD1 Degrader-1.
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DC78292 MS44
MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors.
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DC78283 FLT3/JAK2/BRD4 ligand-1
FLT3/JAK2/BRD4 ligand-1 is a FLT3/JAK2/BRD4 ligand. FLT3/JAK2/BRD4 ligand-1 can be used for synthesis PROTAC FLT3/JAK2/BRD4 Degrader-1.
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DC78280 AF151
AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML).
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DC78279 (S,R,S)-AHPC-CO-C2-phenylboronic acid
(S,R,S)-AHPC-CO-C2-phenylboronic acid is an E3 ligase ligand-linker conjugate that incorporates the VH032-based VHL ligand and linker. (S,R,S)-AHPC-CO-C2-phenylboronic acid can be used for synthesis of PROTAC AF151.
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DC78270 JY-21
JY-21 is a BRD4 PROTAC degrader with a DC50 of 3.797 μM. JY-21 has a potent anticancer activity against MDA-MB-231 cells.
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