2. Signaling Pathways
  3. PROTAC
  4. PROTACs

PROTACs

PROTACs

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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:

PROTACs Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-176857
    PROTAC STAT6 degrader-1 3077464-21-9 99.55%
    PROTAC STAT6 degrader-1 (Compound I-2) is a potent STAT6 PROTAC degrader with a DC50 <1 nM. PROTAC STAT6 degrader-1 inhibits STAT6 activity with an IC50 of <0.1 pM. PROTAC STAT6 degrader-1 can be used for inflammatory and cancers research, such as non-small cell lung cancer (NSCLC).
    PROTAC STAT6 degrader-1
  • HY-160259
    VEGFR-2-IN-39 2353417-86-2 99.09%
    VEGFR-2-IN-39 (PROTAC-5) is a PROTAC targeting VEGFR-2 (IC50: 208.6 nM). VEGFR-2-IN-39 has low toxicity.VEGFR-2-IN-39 inhibits the proliferation of EA.hy926, one of HUVECs, in a concentration-dependent manner, with an IC50 of 38.65 µM.
    VEGFR-2-IN-39
  • HY-144995
    BSJ-02-162 2139329-47-6 98.07%
    CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader. CDK4/6-IN-11 consists of a thalidomide-based E3 ligase ligand (blue part) Thalidomide-NH-CH2-COOH (HY-131717), a target protein ligand (red part) Palbociclib (HY-50767), and a PROTAC linker (black part) Boc-NH-C4-Br (HY-W007803). E3 ligase ligand and linker can form Thalidomide-NH-amido-C4-Br (HY-170307).
    BSJ-02-162
  • HY-157581
    MS39 2675490-92-1 99.89%
    MS39 (compound 6) is a PROTAC targeting EGFR. MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells.
    MS39
  • HY-156568B
    SMD-3040 formate 99.78%
    SMD-3040 formate is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 formate can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 formate can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
    SMD-3040 formate
  • HY-145815A
    JPS014 TFA 98.12%
    JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
    JPS014 TFA
  • HY-155218
    TMX-2172 2488892-09-5 99.38%
    TMX-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.
    TMX-2172
  • HY-139185
    PROTAC ERRα Degrader-3 2306388-65-6 98.82%
    PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
    PROTAC ERRα Degrader-3
  • HY-171768
    SK2187 3038446-91-9
    SK2187 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 (Pink: AURKA ligand: MK-5108 (HY-13252); Blue: E3 ligand (HY-103597); Black: Linker: Amino-PEG3-alcohol (HY-W015088)).
    SK2187
  • HY-170329
    PROTAC AR Degrader-8 3044108-04-2 99.98%
    PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC50s of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 values of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer.
    PROTAC AR Degrader-8
  • HY-136001
    PROTAC α-synuclein degrader 3 2412273-77-7 99.61%
    PROTAC α-synuclein degrader 3 (Compound 5) is a selective α-synuclein PROTAC degrader. PROTAC α-synuclein degrader 3 can promote the ubiquitination and degradation of α-synuclein. PROTAC α-synuclein degrader 3 can be used for Parkinson's disease research (Pink: target protein ligand (HY-W278021); Black: linker; HY-133302; Blue: E3 ligase VHL ligand (HY-112078)).
    PROTAC α-synuclein degrader 3
  • HY-168660
    CPD-10 3055471-57-0 98.59%
    CPD-10 is a potent CCND1 and CDK4 PROTAC degrader. CPD-10 exhibits anti-proliferative effects on tumor cells and can also induce apoptosis. CPD-10 can be used for the study of breast cancer and lung cancer.
    CPD-10
  • HY-149924
    CST626 3033993-13-1 99.60%
    CST626 (Compound 9) is a pan-IAP degrader PROTAC. CST626 degrades XIAP, cIAP1 and cIAP2 with DC50s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively.
    CST626
  • HY-160415
    WD6305 3066823-45-5 98.98%
    WD6305 is a potent and selective METTL3-METTL14 PROTAC degrader. WD6305 has DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. WD6305 inhibits m6A modification and proliferation of AML cells, and induces apoptosis. WD6305 has antitumor activity.(Pink: UZH2 (HY-115717); Black: Linker; Blue: VHL ligand (HY-150803))
    WD6305
  • HY-157570
    Anti-inflammatory agent 70 2767427-87-0
    Anti-inflammatory agent 70 (N-Me-SP23) is a STING protein PROTAC degrader and inhibits the STING signaling pathway. Anti-inflammatory agent 70 has anti-inflammatory activity. (Pink: STING inhibitor (HY-47709); Black: linker (HY-W008296); Blue: CRBN Ligand (HY-W460193)).
    Anti-inflammatory agent 70
  • HY-158239
    MS181 3037165-65-1 98.36%
    MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717).
    MS181
  • HY-103633
    PROTAC BET Degrader-1 2093386-22-0 99.41%
    PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
    PROTAC BET Degrader-1
  • HY-156111
    ARD-1676 2632305-36-1 99.36%
    ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models.
    ARD-1676
  • HY-153357
    NRX-0492 2416130-57-7 98.30%
    NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC50 ≤ 0.2 nM, DC90 ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 has antitumor effects against chronic lymphocytic leukemia.NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263).
    NRX-0492
  • HY-168439
    HLB-0532259 2566733-45-5 98.30%
    HLB-0532259 is a PROTAC degrader for Aurora-A and N-Myc. HLB-0532259 degrades Aurora-Ain a non-MYCN amplified MCF-7 with a DC50 of 20.2 nM, degrades N-Myc in MYCN amplified cells SK-N-BE and Kelly with DC50 of 179 nM and 229 nM. HLB-0532259 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-168440); Black: linker (HY-W007957); Blue: ligand for E3 ligase Cereblon (HY-41547))
    HLB-0532259
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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