PROTAC

Total: 2437
Updated: 2019-06-28 15:55:20
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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NH-bis(PEG3-t-butyl ester)

NH-bis(PEG3-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1814901-03-5
  • MF: C26H51NO10
  • MW: 537.68
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Hydroxy-PEG1-C2-methyl ester

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

  • CAS Number: 93673-82-6
  • MF: C6H12O4
  • MW: 148.15700
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Fluorescein-PEG4-Acid

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

  • CAS Number: 1807518-76-8
  • MF: C32H34N2O11S
  • MW: 654.684
  • Catalog: PROTAC Linker
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 892.9±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 493.8±37.1 °C
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Propargyl-PEG3-methyl ester

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

  • CAS Number: 2086689-09-8
  • MF: C11H18O5
  • MW: 230.26
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Amino-PEG12-amine

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

  • CAS Number: 361543-12-6
  • MF: C26H56N2O12
  • MW: 588.73
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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N-(Azido-PEG2)-N-Boc-PEG4-NHS ester

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

  • CAS Number: 2093153-95-6
  • MF: C26H45N5O12
  • MW: 619.66
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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N-(Azido-PEG3)-N-Boc-PEG4-acid

N-(Azido-PEG3)-N-Boc-PEG4-acid is a PEG-based PROTAC linker with a terminal azide group and is used in the synthesis of PROTACs[1]

  • CAS Number: 2112731-95-8
  • MF: C24H46N4O11
  • MW: 566.64
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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m-PEG6-2-methylacrylate

m-PEG6-2-methylacrylate is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 90784-86-4
  • MF: C17H32O8
  • MW: 364.43
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Propargyl-PEG3-phosphonic acid ethyl ester

Propargyl-PEG3-phosphonic acid diethyl ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 1052678-30-4
  • MF: C13H25O6P
  • MW: 308.31
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Azido-PEG4-propargyl

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

  • CAS Number: 1192590-91-2
  • MF: C11H19N3O4
  • MW: 257.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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PROTAC BRD4 Degrader-2

PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC50 of 14.2 nM against BRD4 BD1[1].

  • CAS Number: 2185795-53-1
  • MF: C40H39N9O7
  • MW: 757.79
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Propargyl-PEG8-Boc

Propargyl-PEG7-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055014-96-3
  • MF: C24H44O10
  • MW: 492.600
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 528.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 220.3±28.8 °C
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Thalidomide-O-C5-NH2 hydrochloride

Thalidomide-O-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[1].

  • CAS Number: 2419145-66-5
  • MF: C18H22ClN3O5
  • MW: 395.84
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Ald-PEG1-t-butyl ester

Ald-PEG1-C2-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2100306-48-5
  • MF: C10H18O4
  • MW: 202.25
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Thalidomide-PEG4-NH2 hydrochloride

Thalidomide-PEG4-NH2 hydrochloride 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: 2387510-82-7
  • MF: C21H28ClN3O8
  • MW: 485.92
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Aminooxy-PEG4-propargyl

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

  • CAS Number: 1835759-78-8
  • MF: C11H21NO5
  • MW: 247.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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N-(m-PEG4)-N'-(PEG2-acid)-Cy5

N-(m-PEG4)-N'-(PEG2-acid)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2107273-24-3
  • MF: C41H57ClN2O8
  • MW: 741.35
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Azido-PEG7-CH2COOH

Azido-PEG7-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1446411-32-0
  • MF: C16H31N3O9
  • MW: 409.43
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Propargyl-PEG3-phosphonic acid

Propargyl-PEG3-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 1714139-62-4
  • MF: C9H17O6P
  • MW: 252.20
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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S-Acetyl-PEG3-azide

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

  • CAS Number: 1310827-26-9
  • MF: C10H19N3O4S
  • MW: 277.341
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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N-(Azido-PEG3)-N-Boc-PEG4-NHS ester

N-(Azido-PEG4)-N-Boc-PEG4-NHS ester is a PEG-based PROTAC linker with a terminal azide group. N-(Azido-PEG4)-N-Boc-PEG4-NHS ester is used in the synthesis of PROTACs[1]

  • CAS Number: 2112731-96-9
  • MF: C28H49N5O13
  • MW: 663.71
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Boc-NH-PEG7-acid

Boc-NH-PEG7-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055044-68-1
  • MF: C22H43NO11
  • MW: 497.577
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 598.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 315.7±30.1 °C
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HO-PEG16-OH

HO-PEG16-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 6812-36-8
  • MF: C32H66O17
  • MW: 722.85600
  • Catalog: PROTAC Linker
  • Density: 1.116g/cm3
  • Boiling Point: 714.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 386.1ºC
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Thalidomide 4'-ether-alkylC2-amine hydrochloride

Pomalidomide-PEG1-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology[1].

  • CAS Number: 2341840-99-9
  • MF: C15H16ClN3O5
  • MW: 353.76
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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N-(Amino-PEG1)-N-bis(PEG2-propargyl)

N-(Amino-PEG1)-N-bis(PEG2-propargyl) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2100306-47-4
  • MF: C18H32N2O5
  • MW: 356.457
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 443.9±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 222.2±27.3 °C
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DBCO-PEG9-DBCO

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

  • CAS Number: 2353409-50-2
  • MF: C58H70N4O13
  • MW: 1031.20
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Benzyl-PEG2-ethanol

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

  • CAS Number: 2055300-50-8
  • MF: C13H20O3
  • MW: 224.30
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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2-(3,6-Bis(dimethylamino)xanthylium-9-yl)-5-((2-(2-(2-(2-(4-(6-methyl-1,2,4,5-tetrazin-3-yl)phenoxy)ethoxy)ethoxy)ethoxy)ethyl)carbamoyl)benzoate

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

  • CAS Number: 2163772-19-6
  • MF: C42H45N7O8
  • MW: 775.85
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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N-(Amino-PEG4)-N-bis(PEG4-t-butyl ester)

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

  • CAS Number: 2093153-97-8
  • MF: C40H80N2O16
  • MW: 845.07
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Acid-C2-PEG3-NHS ester

Acid-C2-PEG3-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1835759-79-9
  • MF: C14H21NO9
  • MW: 347.318
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 516.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 265.9±32.9 °C
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