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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HO-PEG5-CH2COOH

HO-PEG5-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 52026-48-9
  • MF: C12H24O8
  • MW: 296.31
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyloxy-C5-PEG1

Benzyloxy-C5-PEG1 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 159028-70-3
  • MF: C14H22O3
  • MW: 238.32
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-cis-4-hydroxy-D-proline methyl ester

N-Boc-cis-4-hydroxy-D-proline methyl ester is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-Boc-cis-4-hydroxy-D-proline methyl ester is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1

  • CAS Number: 114676-69-6
  • MF: C11H19NO5
  • MW: 245.27200
  • Catalog: ADC Linker
  • Density: 1.216g/cm3
  • Boiling Point: 335.2ºC at 760mmHg
  • Melting Point: 80 °C
  • Flash Point: 156.6ºC

Boc-trans-D-Hyp-OMe

Boc-trans-D-Hyp-OMe is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Boc-trans-D-Hyp-OMe is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].

  • CAS Number: 135042-17-0
  • MF: C11H19NO5
  • MW: 245.272
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 387.6±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 188.2±27.9 °C

Pentaethylene glycol di(p-toluenesulfonate)

Pentaethylene glycol di(p-toluenesulfonate) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 41024-91-3
  • MF: C24H34O10S2
  • MW: 546.65100
  • Catalog: PROTAC Linker
  • Density: 1.26
  • Boiling Point: 661.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 353.8ºC

2,3,4,6-Tetra-o-acetyl-alpha-galactosylpyranosyl bromide

2,3,4,6-Tetra-o-acetyl-alpha-galactosylpyranosyl bromide is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 529493-92-3
  • MF: C14H19BrO9
  • MW: 411.20
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia[1].

  • CAS Number: 2347517-69-3
  • MF: C41H46N6O6S
  • MW: 750.91
  • Catalog: HIF/HIF Prolyl-Hydroxylase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SCO-PEG8-NHS

SCO-PEG8-NHS SCO is a PROTAC linker and belongs to the PEG class. SCO-PEG8-NHS SCO contains SCO and NHS esters that can be covalently bound to amino groups, respectively. SCO is often used to react with amino acid residues of proteins or peptides, particularly lysine.

  • CAS Number: 2143968-68-5
  • MF: C32H52N2O14
  • MW: 688.76
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Mal-N-bis(PEG4-acid)

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

  • CAS Number: 2100306-52-1
  • MF: C29H48N2O15
  • MW: 664.70
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC PTPN2 degrader-1

PROTAC PTPN2 degrader-1 (compound example 77) is a potent PTPN2 degrader. PROTAC PTPN2 degrader-1 has the potential for the research of cancer or metabolic disease[1].

  • CAS Number: 2655638-07-4
  • MF: C33H27FN6O8S
  • MW: 686.67
  • Catalog: Phosphatase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chloro-PEG2-Boc

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

  • CAS Number: 1442085-43-9
  • MF: C10H19ClO4
  • MW: 238.71
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-O-C8-NH2

Thalidomide-O-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 1957235-91-4
  • MF: C21H27N3O5
  • MW: 401.46
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG2-alcohol

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

  • CAS Number: 57641-66-4
  • MF: C4H9BrO2
  • MW: 169.01700
  • Catalog: PROTAC Linker
  • Density: 1.514±0.06 g/cm3
  • Boiling Point: 228.9±15.0 °C
  • Melting Point: N/A
  • Flash Point: N/A

Lipoamido-PEG4-acid

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

  • CAS Number: 1314378-10-3
  • MF: C19H35NO7S2
  • MW: 453.614
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 650.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 347.3±31.5 °C

Target Protein-binding moiety 4

Target Protein-binding moiety 4 is a BRD4(1) inhibitor with an IC50 of 7.9 μM.

  • CAS Number: 1300019-38-8
  • MF: C20H17ClN4O3
  • MW: 396.83
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MS177

MS177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models.

  • CAS Number: 2225938-86-1
  • MF: C48H55N11O8
  • MW: 914.037
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 14

E3 ligase Ligand-Linker Conjugates 14 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 1957236-21-3
  • MF: C25H31F3N4O11
  • MW: 620.53
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG6-PFP ester

Mal-PEG6-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1599486-33-5
  • MF: C25H30F5NO10
  • MW: 599.498
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 623.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 330.6±31.5 °C

1,3,4,6-Tetra-O-acetyl-2-[(azidoacetyl)amino]-2-deoxy-β-D-galactopyranos

Ac4GalNAz is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 653600-56-7
  • MF: C16H22N4O10
  • MW: 430.37
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KB02-COOH

KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 (HY-129917) and KB02-SLF (HY-129610)[1].

  • CAS Number: 2375196-30-6
  • MF: C13H14ClNO4
  • MW: 283.71
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG5-NHS ester

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

  • CAS Number: 1433996-86-1
  • MF: C17H28N4O9
  • MW: 432.426
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG8-azide

Azido-PEG8-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 361543-07-9
  • MF: C18H36N6O8
  • MW: 464.514
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

THP-PEG3-OH

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

  • CAS Number: 60221-37-6
  • MF: C11H22O5
  • MW: 234.28900
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-C7-COOH

Pomalidomide-C7-COOH is a synthesized E3 ligase cereblon ligand-linker conjugate. Pomalidomide-C7-COOH is an intermediate for the synthesis of PROTAC BCL-XL degraders[1].

  • CAS Number: 2225940-51-0
  • MF: C21H25N3O6
  • MW: 415.44
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2,5,8,11,14,17-Hexaoxanonadecan-19-ol

Hexaethylene glycol monomethyl ether is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 23601-40-3
  • MF: C13H28O7
  • MW: 296.357
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 375.6±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 180.9±26.5 °C

Bis-sulfone-PEG4-DBCO

Bis-sulfone-PEG4-DBCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1854034-70-0
  • MF: C54H59N3O12S2
  • MW: 1006.19
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3,6,9,12,15,18,21-Heptaoxatritriacontan-1-ol

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

  • CAS Number: 3055-97-8
  • MF: C26H54O8
  • MW: 494.702
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 553.9±45.0 °C at 760 mmHg
  • Melting Point: 27-29 °C
  • Flash Point: 288.8±28.7 °C

N-(Azido-PEG3)-N-(PEG2-amine)-PEG3-acid

N-(Azido-PEG3)-N-(PEG2-amine)-PEG3-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2183440-70-0
  • MF: C24H47N5O11
  • MW: 581.66
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ARD-2051

ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer[1].

  • CAS Number: 2632305-17-8
  • MF: C43H45ClN8O5
  • MW: 789.32
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 Ligand-Linker Conjugate 10

An E3 ligase ligand-linker conjugate for PROTAC.

  • CAS Number: 1957236-22-4
  • MF: C25H34N4O10
  • MW: 550.565
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A