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 (1321)
Related Products (1321)
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Antibodies (1)
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PROTACs Isoform Comparison
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LYP-8
0 ImagesLYP-8 is an intracellular nicotinamide phosphoribosyltransferase (iNAMPT) inhibitor with an IC50 of 0.76 μM, a reducing agent, and a tumor growth inhibitor. LYP-8 recruits VHL E3 ligase to induce iNAMPT polyubiquitination and proteasome-dependent degradation, and inhibits iNAMPT enzymatic activity. LYP-8 reduces eNAMPT levels by degrading iNAMPT to decrease eNAMPT secretion. LYP-8 reduces intracellular NAD+ levels in cancer cells and proinflammatory cytokine levels (IL-6, TNF-α) in tumor tissue and serum. LYP-8 can be used for the research of colon cancer.
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(Rac)-P1D-34
0 ImagesPROTAC PIN1 degrader-2 (1) is a PROTAC-based PIN1 degrader (Pink: PIN1 ligand HY-171442, Blue: cereblon ligand Thalidomide (HY-14658), Black: linker HY-W014883). PROTAC PIN1 degrader-2 (1) possesses anti-cancer activity, with IC50 values of 2248 nM (MV-4-11 cells), 3984 nM (MOLM-13), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60) and 3925 nM (HL-60) respectively.
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FC-14369
0 ImagesCat. No.: HY-171860CAS No.: 3066894-28-5FC-14369 is a PROTAC degrader targeting the HIV-1 Nef protein, with a DC50 value of 160 nM. Through its bifunctional structure, FC-14369 binds to Nef and the Cereblon E3 ubiquitin ligase, induces Nef ubiquitination and proteasomal degradation, restores the expression of cell-surface CD4 and MHC-I, and inhibits HIV-1 replication. FC-14369 can be used in research on HIV infection and AIDS. FC-14369 is applicable to studies related to HIV-1 infection.
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PROTAC Chk1 degrader-1
0 ImagesPROTAC Chk1 degrader-1 is a Chk1-targeting PROTAC.PROTAC Chk1 degrader-1 recruits the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of Chk1.PROTAC Chk1 degrader-1 exhibits Chk1 degradation activity in malignant melanoma cells without showing a hook effect.PROTAC Chk1 degrader-1 can be used for the research of malignant melanoma.
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PROTAC CDK2/4/6 Degrader-2
0 ImagesCat. No.: HY-185121CAS No.: 2541626-49-5PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research.
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LC-MF-4
0 ImagesCat. No.: HY-174981Purity: 98.05%LC-MF-4 is a selective FGFR3 PROTAC degrader with a DC50 of 30.89 nM in KMS-11 cells. LC-MF-4 inhibits the metabolic function of FGFR3-TACC3 fusion positive cancers with reduction of ATP synthesis and inhibition of mitochondrial biogenesis genes. LC-MF-4 has potent antitumor activity in the Ba/F3-FGFR3-TACC3 xenograft mice model. LC-MF-4 can be used for FGFR3-altered cancers like bladder cancer and urothelial carcinoma (UC) research. Pink: FGFR3 ligand (HY-175414); Blue: VHL ligase ligand (HY-125905); Black: linker (HY-Y1224)
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PROTAC G9a/GLP degrader 1
0 ImagesCat. No.: HY-178065Purity: 98.22%PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468)).
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DDC-01-163
0 ImagesDDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer.
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CG428-NEG
0 ImagesCat. No.: HY-157542CAS No.: 2714560-39-9CG428-NEG is the negative control of PROTAC CG428 (HY-137465). CG428-NEG binds to TRKA, TRKB and TRKC with high affinity, with Kd values of 0.88 nM, 4.8 nM and 59.8 nM, respectively. CG428-NEG inhibits the growth of cancer cells and reduces the level of TPM3-TRKA fusion protein in cancer cells. CG428-NEG can be used in the research of colorectal cancer.
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PROTAC AR Degrader-4 TFA
0 ImagesCat. No.: HY-111848APurity: 99.26%PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
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ML 2-14
0 ImagesCat. No.: HY-132991Purity: 99.43%ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487). ML 2-14 can be used for breast cancer-related research.
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A947
0 ImagesCat. No.: HY-148381CAS No.: 2378056-80-3A947 is a VHL-based SMARCA2 PROTAC degrader with a DC50 of 39 pM and a Kd of 93 nM for human SMARCA2. A947 recruits SMARCA2 to the VHL E3 ubiquitin ligase for ubiquitination modification, mediates its degradation via the proteasome, and exerts selective degradation effects on SMARCA4 and PBRM1. A947 induces G1 cell cycle arrest, inhibits transcription, and exerts growth inhibitory effects in SMARCA4G12C-mutant cancer cells. A947 acts synergistically with MCL1 inhibitors to induce apoptosis in SMARCA4G12C-mutant cancer cells. A947 can be used in studies related to SMARCA4G12C-mutant non-small cell lung cancer and non-small cell lung cancer.
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(rel)-PROTAC ERRα Degrader-1
0 ImagesCat. No.: HY-128838APurity: 98.18%
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PROTAC HPK1 Degrader-5
0 ImagesCat. No.: HY-175547CAS No.: 3108744-13-1PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy.
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PROTAC RNF4 degrader-1
0 ImagesCat. No.: HY-181692Purity: 98.09%PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma.
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MS15
0 ImagesCat. No.: HY-151613CAS No.: 3035638-40-2
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PROTAC AR Degrader-4
0 ImagesCat. No.: HY-111848CAS No.: 1351169-31-7PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
