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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TD-802

TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research[1].

  • CAS Number: 2760703-21-5
  • MF: C52H61ClN10O6
  • MW: 957.56
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(+)-Biotin-SLC

(+)-Biotin-SLC is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1864003-57-5
  • MF: C23H41N3O4S
  • MW: 427.601
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 730.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 395.5±28.7 °C

Mal-PEG2-NH2 TFA

Mal-PEG2-NH2 (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 660843-23-2
  • MF: C12H17F3N2O6
  • MW: 342.26800
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG4-C2-amine

Amino-PEG4-C2-amine is a PEG-based (4 units) PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 68960-97-4
  • MF: C10H24N2O4
  • MW: 236.30900
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: 139 °C/0.2 mmHg
  • Melting Point: N/A
  • Flash Point: 157 °C

Bis-propargyl-PEG3

Bis-propargyl-PEG3 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG3 is used in the synthesis of zinc-dipicolylamine (ZnDPA) complexes with antiplasmodial activity[1] [2].

  • CAS Number: 126422-58-0
  • MF: C12H18O4
  • MW: 226.26900
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-dPEG13-PFP ester

Bis-PEG9-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1334170-00-1
  • MF: C34H40F10O13
  • MW: 846.657632
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG2-MS

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

  • CAS Number: 150272-33-6
  • MF: C12H18O5S
  • MW: 274.33
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-4-NH-PEG1-NH2 TFA

Thalidomide-4-NH-PEG1-NH2 TFA is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-4-NH-PEG1-NH2 TFA acts as a ligand for Cereblon to recruit CRBN protein. Thalidomide-4-NH-PEG1-NH2 TFA is a key intermediate in the synthesis of CRBN-based PROTAC molecules.

  • CAS Number: 2490499-21-1
  • MF: C19H21F3N4O7
  • MW: 474.39
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-Bromobutylphosphonic acid

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

  • CAS Number: 1190-14-3
  • MF: C4H10BrO3P
  • MW: 216.99800
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 129 °C
  • Flash Point: N/A

t-Boc-Aminooxy-PEG4-NHS ester

t-Boc-Aminooxy-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2401831-99-8
  • MF: C20H34N2O11
  • MW: 478.49
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-methyl-N-(t-Boc)-PEG4-acid

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

  • CAS Number: 1260431-01-3
  • MF: C17H33NO8
  • MW: 379.446
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 488.2±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 249.1±28.7 °C

2-Bromo-22-dimethyl-acetamido-PEG3-acid

2-Bromo-22-dimethyl-acetamido-PEG3-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2279944-67-9
  • MF: C13H24BrNO6
  • MW: 370.24
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

dBRD9 dihydrochloride

dBRD9 dihydrochloride is a potent and selective degrader (PROTAC) of BRD9 with IC50 of 56.6 nM in MOLM-13 cells.dBRD9 is composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide.dBRD9 does not degrade BRD4 or BRD7 at concentrations up to 5 uM.dBRD9 exhibits antiproliferative effects in human AML cell lines.

  • CAS Number: 2341840-98-8
  • MF: C40H47Cl2N7O10
  • MW: 856.755
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HS-PEG6-CH2CH2-Boc

HS-PEG6-CH2CH2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1818294-40-4
  • MF: C19H38O8S
  • MW: 426.565
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 488.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 337.6±16.6 °C

Phthalamide-PEG3-azide

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

  • CAS Number: 134179-44-5
  • MF: C16H20N4O5
  • MW: 348.35400
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCO-C3-PEG3-C3-amine

TCO-C3-PEG3-C3-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2028288-77-7
  • MF: C19H36N2O5
  • MW: 372.50
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2,5,8,11,14,17,20-Heptaoxadocosan-22-oic acid

m-PEG6-O-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 75427-75-7
  • MF: C15H30O9
  • MW: 354.39
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-propargyl-PEG8

Bis-propargyl-PEG8 (compound 16e) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1092554-87-4
  • MF: C22H38O9
  • MW: 446.532
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 495.5±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 187.0±27.2 °C

Ald-Ph-PEG2-amine TFA

Ald-Ph-amido-C2-PEG2-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055013-56-2
  • MF: C14H20N2O4
  • MW: 280.32
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

XY028-133

XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, extracted from patent WO2018106870A1[1].

  • CAS Number: 2229974-73-4
  • MF: C53H67N11O7S
  • MW: 1002.23
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

M-Peg3-sulfone-peg3-t-butyl ester

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

  • CAS Number: 2055041-00-2
  • MF: C20H40O10S
  • MW: 472.59
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH-bis(C1-PEG1-Boc)

NH-bis(C1-PEG1-Boc) is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2171072-53-8
  • MF: C17H33NO6
  • MW: 347.45
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC VEGFR-2 degrader-1

The compound is a new angiogenesis inhibitor, which can be used to normalize abnormal blood vessels and effectively deliver drugs.

  • CAS Number: 2601594-19-6
  • MF: C52H61N9O6S
  • MW: 940.16
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG2-amine TFA

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

  • CAS Number: 660843-22-1
  • MF: C10H16N2O4
  • MW: 228.25
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG4-Glu(OH)-NH-m-PEG24

Mal-PEG4-Glu(OH)-NH-m-PEG24 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2204309-09-9
  • MF: C72H134N4O35
  • MW: 1615.84
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-Azidohomoalanine hydrochloride

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

  • CAS Number: 942518-29-8
  • MF: C4H9ClN4O2
  • MW: 180.59300
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Alkynyl myristic acid

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

  • CAS Number: 82909-47-5
  • MF: C14H24O2
  • MW: 224.339
  • Catalog: PROTAC Linker
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 341.6±15.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 165.8±15.1 °C

Lenalidomide-6-F

Lenalidomide-6-F is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-6-F can be connected to the ligand for protein by a linker to form PROTAC[1].

  • CAS Number: 2468780-87-0
  • MF: C13H11FN2O3
  • MW: 262.24
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG10-amine

Propargyl-PEG10-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 2112737-25-2
  • MF: C23H45NO10
  • MW: 495.60
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-(Biotinamido)pentylazide

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

  • CAS Number: 1349190-76-6
  • MF: C15H26N6O2S
  • MW: 354.47
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A