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
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PROTACs Related Products (1355)
Related Products (1355)
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Antibodies (1)
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PROTACs Isoform Comparison
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JHK-02-108-2
0 ImagesCat. No.: HY-184910JHK-02-108-2 is a PROTAC degrader targeting CDK6, with an EC50 of 0.22 μM and a Kd of 1.9 μM. JHK-02-108-2 selectively promotes CRBN-dependent ubiquitination and proteasomal degradation of CDK6. JHK-02-108-2 induces sustained cell cycle arrest at the G1 phase. JHK-02-108-2 reduces the phosphorylation level of retinoblastoma protein. JHK-02-108-2 can be used in research related to acute myeloid leukemia and glioblastoma.
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PROTAC EZH2 Degrader-42
0 ImagesCat. No.: HY-181411CAS No.: 3093642-42-0
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SIAIS056
0 ImagesCat. No.: HY-180969CAS No.: 2378581-37-2SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research.
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PROTAC SMARCA2 degrader-29
0 ImagesCat. No.: HY-168246CAS No.: 2865193-25-3
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PROTAC TSSK1 Degrader-1
0 ImagesCat. No.: HY-184428PROTAC TSSK1 Degrader-1 is a TSSK1 PROTAC degrader with a DC50 of 10.8 nM and an IC50 of 56.8 nM. PROTAC TSSK1 Degrader-1 reduces sperm motility and impairs in vitro fertilization capacity. PROTAC TSSK1 Degrader-1 undergoes metabolic N-dealkylation and exhibits high efflux properties. PROTAC TSSK1 Degrader-1 is applicable to studies related to male fertility.
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ERB-2
0 ImagesCat. No.: HY-180850ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer.
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SGI-1776-VHL-02-epimer
0 ImagesCat. No.: HY-186146ACAS No.: 3013618-85-1Synonyms: SGI-1776-cis-VHL-02SGI-1776-VHL-02-epimer (SGI-1776-cis-VHL-02) is an epimer control compound of with SGI-1776-VHL-02 (HY-186146). SGI-1776-VHL-02-epimer has an inverted stereocenter in the critical hydroxyl-proline group in the VHL ligand. SGI-1776-VHL-02-epimer cannot trigger the VHL E3 ligase complex and does not degrade PIM1.
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PROTAC ALK degrader-3
0 ImagesCat. No.: HY-168551PROTAC ALK degrader-3 is an orally active ALK PROTAC degrader with a DC50 of 119.33 nM in Karpas 299 cells. PROTAC ALK degrader-3 induces the degradation of ALK fusion proteins via the ubiquitin-proteasome system. PROTAC ALK degrader-3 induces NPM-ALK degradation and inhibits the expression of p-ALK and p-STAT3. PROTAC ALK degrader-3 inhibits cancer cell proliferation and suppresses the growth of xenografts in vivo. PROTAC ALK degrader-3 can be used for the research of ALK-positive cancers (e.g., anaplastic large cell lymphoma).
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SJ11646
0 ImagesSJ11646 is a LCK PROTAC degrader with a DC50 value of 0.00838 pM against LCK. SJ11646 recruits CRBN and LCK to form a ternary complex, inducing cereblon-mediated proteasomal degradation of LCK. SJ11646 induces cytotoxicity in T-ALL cells, but such cytotoxicity is reduced in cells harboring the LCKT316I mutation. SJ11646 can be used in studies related to T-cell acute lymphoblastic leukemia.
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A031
0 ImagesCat. No.: HY-148777CAS No.: 2682255-44-1A031 is a PROTAC degrader targeting the androgen receptor. A031 induces time-dependent degradation of androgen receptor protein. A031 exerts tumor growth inhibitory effects in a zebrafish model xenografted with human prostate cancer cells. A031 can be used in studies related to prostate cancer.
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GDCNF-11
0 ImagesCat. No.: HY-169133CAS No.: 2991588-80-6GDCNF-11 is a type of HSP90 interaction-mediated protein degradation chimera (HIM-PROTAC) degrader that targets and degrades GPX4, with a DC50 of 0.08 μM. GDCNF-11 mediates the ubiquitination and proteasome-dependent degradation of GPX4 by recruiting GPX4 to form a ternary complex with HSP90, increases intracellular lipid peroxides and ROS, and ultimately triggers Ferroptosis. GDCNF-11 inhibits tumor growth in mouse models, downregulates GPX4 protein in xenograft tumors, and upregulates the lipid peroxidation marker. GDCNF-11 can be used for the research of fibrosarcoma.
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PTOTAC HSD17B13 degrader 1
0 ImagesCat. No.: HY-159651CAS No.: 3046195-01-8
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PROTAC PRMT1 degrader-1
0 ImagesCat. No.: HY-182275PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma.
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dCBP-30
0 ImagesCat. No.: HY-184556dCBP-30 is an orally active, selective and dual-acting CBP/p300 PROTAC degrader with DC50 values of 0.05 nM (CBP) and 0.04 nM (p300), respectively. dCBP-30 reduces the acetylation levels of histone substrates H3K27, H3K18, H2BK5 and H2BK20, downregulates multiple myeloma-specific dependency programs, and induces multiple myeloma cell apoptosis. dCBP-30 triggers tumor regression and prolongs survival in multiple myeloma xenograft mouse models, and exhibits synergistic antiproliferative activity with dexamethasone. dCBP-30 can be used for the research of multiple myeloma.
