PROTACs or Proteolysis Targeting Chimeric Molecules are heterobifunctional nanomolecules that theoretically target any protein for ubiquitination and degradation. In terms of the structure, PROTACs consist of one moiety which is recognized by the E3 ligase. This moiety is then chemically and covalently linked to a small molecule or a protein that recognizes the target protein. The trimeric complex formation leads to the transfer of ubiquitins to the target protein.

By removing target proteins directly rather than merely blocking them, PROTACs can provide multiple advantages over small molecule inhibitors, which can require high systemic exposure to achieve sufficient inhibition, often resulting in toxic side effects and eventual drug resistance. PROTAC molecules possess good tissue distribution and the ability to target intracellular proteins, thus can be directly applied to cells or injected into animals without the use of vectors.

Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases, such as cancer, driven by the aberrant expression of a disease-causing protein. In addition to the use of PROTACs for the treatment of human disease, these molecules provide a chemical genetic approach to “knock down” proteins to study their function. Currently, there are several small molecule inhibitors that have been found to show good biological activity by specifically targeting BET, estrogen receptor (ER), androgen receptor, etc.

References:
[1] Sakamoto KM. Pediatr Res. 2010 May;67(5):505-8.
[2] Neklesa TK, et al. Pharmacol Ther. 2017 Jun;174:138-144.


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MS4078

MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19 nM for binding affinity to ALK[1].

  • CAS Number: 2229036-62-6
  • MF: C45H52ClN9O8S
  • MW: 914.47
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BocNH-PEG6-CH2CH2NH2

Boc-NH-PEG6-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1091627-77-8
  • MF: C19H40N2O8
  • MW: 424.53000
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-Tri-(carboxyethoxymethyl)-methane

Amino-Tri-(carboxyethoxymethyl)-methane is a cleavable PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Amino-Tri-(carboxyethoxymethyl)-methan is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 174362-95-9
  • MF: C13H23NO9
  • MW: 337.32
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG8-Tos

Tos-PEG8-m is a derivative of silybin ethers, extracted from patent CN105037337A (compound III-d). Tos-PEG8-m is a PEG-based PROTAC linker can be used in the synthesis of Silymarin (HY-W043277)[1].

  • CAS Number: 82217-01-4
  • MF: C24H42O11S
  • MW: 538.65
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ald-C2-PEG4-azide

Ald-C2-PEG4-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2030118-14-8
  • MF: C11H21N3O5
  • MW: 275.302
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-amido-PEG9-amine

Boc-amido-PEG9-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 890091-43-7
  • MF: C25H52N2O11
  • MW: 556.68700
  • Catalog: PROTAC Linker
  • Density: 1.082g/cm3
  • Boiling Point: 609.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 322.6ºC

m-PEG2-amido-Ph-NH2

m-PEG2-amido-Ph-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1284417-66-8
  • MF: C12H18N2O3
  • MW: 238.28
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 10

E3 ligase Ligand-Linker Conjugates 10 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 1835705-57-1
  • MF: C32H47ClN4O6S
  • MW: 651.26
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AM-Imidazole-PA-Boc

AM-Imidazole-PA-Boc is a PROTAC linker, which refers to the alkyl chain composition. AM-Imidazole-PA-Boc can be used in the synthesis of a series of PROTAC IRAK4 degrader-1 (HY-129966)[1].

  • CAS Number: 2357108-99-5
  • MF: C12H22N4O2
  • MW: 254.33
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-NH-C5-NH2 hydrochloride

Thalidomide-NH-C5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

  • CAS Number: 2375194-03-7
  • MF: C18H23ClN4O4
  • MW: 394.85
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ARCC 4

ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1].

  • CAS Number: 1973403-00-7
  • MF: C53H56F3N7O7S2
  • MW: 1024.18
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-C5-Dovitinib

Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD+ acute myeloid leukemia[1].

  • CAS Number: 2732969-67-2
  • MF: C39H38FN9O6
  • MW: 747.77
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,1,1-Trifluoroethyl-PEG4-alcohol

1,1,1-Trifluoroethyl-PEG4-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1807512-41-9
  • MF: C10H19F3O5
  • MW: 276.250
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 324.8±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 152.6±23.0 °C

Azido-PEG8-TFP ester

Azido-PEG8-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1818294-49-3
  • MF: C25H37F4N3O10
  • MW: 615.569
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG3-PFP ester

Hydroxy-PEG3-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1807537-40-1
  • MF: C15H17F5O6
  • MW: 388.284
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 440.3±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 220.1±28.7 °C

2-Propanone, 1-(2-methoxyethoxy)- (9CI)

PROTAC Linker 28 is a PROTAC linker, which refers to the alkyl chain composition. PROTAC Linker 28 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

  • CAS Number: 88986-89-4
  • MF: C6H12O3
  • MW: 132.15800
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG12-t-butyl ester

Hydroxy-PEG12-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2388521-20-6
  • MF: C31H62O15
  • MW: 674.81
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-C7-NH2 hydrochloride

Pomalidomide-C7-NH2 (Pomalidomide 4'-alkylC7-amine) hydrochloride is an E3 ligase ligand-linker conjugate. Pomalidomide-C7-NH2 hydrochloride can be used for the synthesis of PROTAC[1][2].

  • CAS Number: 2446474-05-9
  • MF: C20H27ClN4O4
  • MW: 422.91
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-[4-(tert-Butoxycarbonyl)piperazino]benzoic acid

Boc-piperazine-benzoic acid is a PROTAC linker and can be used in the synthesis of PROTACs, such as PROTAC androgen receptor (AR) degrader ARD-2128 (HY-13229)[1].

  • CAS Number: 162046-66-4
  • MF: C16H22N2O4
  • MW: 306.357
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 476.9±40.0 °C at 760 mmHg
  • Melting Point: 50ºC
  • Flash Point: 242.2±27.3 °C

Biotin-PEG5-NH-Boc

Biotin-PEG5-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 189209-28-7
  • MF: C27H50N4O9S
  • MW: 606.77
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG2-phosphonic acid diethyl ester

Bromo-PEG2-phosphonic acid diethyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1226767-94-7
  • MF: C10H22BrO5P
  • MW: 333.16
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG36-acid

Amino-PEG36-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2241751-76-6
  • MF: C75H151NO38
  • MW: 1674.99
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromoacetamido-PEG8-acid

Bromoacetamido-PEG8-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1698019-89-4
  • MF: C21H40BrNO11
  • MW: 562.446
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 671.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 359.8±31.5 °C

N-(Azido-PEG2)-N-Boc-PEG4-acid

N-(Azido-PEG2)-N-Boc-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2093153-82-1
  • MF: C22H42N4O10
  • MW: 522.59
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG2-CH2-Boc

Bromo-PEG2-CH2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1807518-63-3
  • MF: C10H19BrO4
  • MW: 283.159
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 316.4±22.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 145.2±22.3 °C

Amino-PEG1-C2-acid

Amino-PEG1-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 144942-89-2
  • MF: C5H11NO3
  • MW: 133.146
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 284.7±20.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 126.0±21.8 °C

Trt-PEG4-C2-acid hydrate

Trt-PEG4-C2-acid (hydrate) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1189873-11-7
  • MF: C30H38O7S
  • MW: 542.68
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG4-azide

Bromo-PEG5-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1951439-37-4
  • MF: C10H20BrN3O4
  • MW: 326.19
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-6

PROTAC IRAK4 degrader-6 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-172[1].

  • CAS Number: 2360530-72-7
  • MF: C42H41F3N12O8
  • MW: 898.85
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tos-PEG3

Tos-PEG3 is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Tos-PEG3 (structure 1) can be used for the synthesis of 3'-aminooxy oligonucleotides solid supports[1].

  • CAS Number: 77544-68-4
  • MF: C13H20O6S
  • MW: 304.35900
  • Catalog: PROTAC Linker
  • Density: 1.234±0.06 g/cm3
  • Boiling Point: 460.0±35.0 °C
  • Melting Point: N/A
  • Flash Point: N/A