PROTACs
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PROTACs Related Products (457)
Related Products (457)
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(Rac)-Vepdegestrant
0 ImagesCat. No.: HY-138642ACAS No.: 2229711-08-2Synonyms: (Rac)-ARV-471; (Rac)-PF-07850327(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
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TKP-5
0 ImagesCat. No.: HY-182370CAS No.: 3076612-97-7TKP-5 is a PROTAC protein degrader targeting BRD4. TKP-5 can binds to BRD2, BRD3, BRD4 and BRDT, with Kd values of 150 nM, 100 nM and 150 nM for the first three proteins respectively. TKP-5 inhibits the production of thymic stromal lymphopoietin and suppresses the expression of IL-33 mRNA. TKP-5 is applicable to studies related to tape-stripping induced skin injury.
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Leu-PEG1-Dasa
0 ImagesCat. No.: HY-180925CAS No.: 3037776-72-7Leu-PEG1-Dasa is a potent BCR-ABL PROTAC degrader with a DC50 of 0.48 nM. Leu-PEG1-Dasa uses a single amino acid as the E3 ligand and belongs to a mini-PROTAC, functioning through the N-terminal canonical pathway. Leu-PEG1-Dasa exhibits potent anti-proliferative activity against K562 cells. Leu-PEG1-Dasa can be used for the study of chronic myeloid leukemia (CML).
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PROTAC BRD9 Degrader-2
0 ImagesCat. No.: HY-145395CAS No.: 2633631-78-2
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PROTAC EGFR degrader 13
0 ImagesCat. No.: HY-158313CAS No.: 2861227-35-0PROTAC EGFR degrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of <0.1 μM. PROTAC EGFR degrader 13 has proliferation inhibitory activity on cell Ba/F3-TEL-EGFR-T790M-L858R-C797S with an IC50 of 15.6 nM. PROTAC EGFR degrader 13 can be used for the study of EGFR-related diseases such as cancer.
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P1D-34
0 ImagesCat. No.: HY-171334AP1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883).
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PROTAC SMARCA2 degrader-21
0 ImagesCat. No.: HY-169272CAS No.: 2891464-61-0
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PROTAC SMARCA2 degrader-17
0 ImagesCat. No.: HY-162747CAS No.: 2568276-43-5
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PROTAC HSP70 Degrader-1
0 ImagesCat. No.: HY-181147PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia.
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Cath-L-dBET1
0 ImagesCat. No.: HY-173257Cath-L-dBET1 is a PROTAC degrader targeting BRD4. Cath-L-dBET1 has an IC50 value of 2.8 μM in MDA-MB-231 cells. Cath-L-dBET1 can be activated by cathepsin L (Cath-L) and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
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PROTAC SMARCA2 degrader-16
0 ImagesCat. No.: HY-162742CAS No.: 2568276-37-7
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MS99-β-Gal
0 ImagesCat. No.: HY-177945CAS No.: 3055593-63-7Synonyms: Gal-MS99MS99-β-Gal (Gal-MS99) is a galactose-modified NPM-ALK PROTAC degrader. MS99-β-Gal is only hydrolyzed by SA-β-gal and esterase in senescent cancer cells, releasing MS99, which specifically degrades the NPM-ALK fusion protein. MS99-β-Gal shows an IC50 of 454.8 nM for aging Karpas 299 cells, significantly lower than that of normal Karpas 299 cells (IC50 = 2.162 μM). MS99-β-Gal can be used for the research of cancer.
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PROTAC PIN1 degrader-2
0 ImagesCat. No.: HY-186218CAS No.: 3083422-10-7PROTAC PIN1 degrader-2 is a PROTAC PIN1 degrader. PROTAC PIN1 degrader-2 reduces PIN1-mediated oncogene expression, upregulates PIN1-inhibited tumor suppressor genes, and exerts killing effects on cancer cells. PROTAC PIN1 degrader-2 inhibits tumor growth in breast cancer mouse xenograft models. PROTAC PIN1 degrader-2 can be used for the research of breast cancer.
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PROTAC SOS1 degrader-5
0 ImagesCat. No.: HY-161173CAS No.: 2836273-61-9PROTAC SOS1 degrader-5 is a potent SOS1 PROTAC degrader with a DC50 value of 13 nM. PROTAC SOS1 degrader-5 induces CRBN-dependent ubiquitination and degradation of SOS1 protein, inhibits the proliferation of KRASG12C-mutated cancer cells, and suppresses tumor growth in xenograft models. PROTAC SOS1 degrader-5 can be used in studies related to KRASG12C-mutated non-small cell lung cancer.
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MRC71
0 ImagesCat. No.: HY-180547CAS No.: 3070832-68-4MRC71 is a TRIMTAC degrader that recruits endogenous TRIM21 E3 ligase at one end and covalently binds to HaloTag-fusion target proteins at the other end. MRC71 selectively degrades oligomeric CAV1- and Cavin1-mEGFP-Halo, but not monomeric mEGFP-Halo, and exhibits a typical concentration-dependent degradation profile with a hook effect. MRC71 can be used to verify TRIMTAC ternary complex formation and state-selective degradation in cells.
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PROTAC MAGL degrader-1
0 ImagesCat. No.: HY-173369PROTAC MAGL degrader-1 is an orally active, moderately blood-brain barrier permeable bifunctional PROTAC (DC50: 60.28 nM) that possesses MAGL degradation activity alongside MDM2 inhibitory activity. PROTAC MAGL degrader-1 recruits E3 ubiquitin ligase MDM2 to mediate ubiquitination of MAGL and subsequent proteasomal degradation. PROTAC MAGL degrader-1 blocks the interaction between MDM2 and P53 and upregulates the expression of tumor suppressor protein P53. PROTAC MAGL degrader-1 is applicable for research on glioblastoma stem cells, melanoma and breast cancer.
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Lw13
0 ImagesCat. No.: HY-162589Lw13 is a Hsp90 PROTAC degrader. Lw13 induces Hsp90 degradation via the ubiquitin-proteasome system, destabilizes client proteins HER2 and AKT, and blocks the activation of the HER2/AKT/mTOR signaling pathway. Lw13 inhibits the metastasis of cervical cancer cells, induces cell cycle arrest and apoptosis (apoptosis). Lw13 exerts synergistic anti-tumor activity with Cisplatin (HY-17394). Lw13 is applicable to cervical cancer-related research.
