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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Bromo-PEG3-C2-phosphonic acid

Bromo-PEG3-C2-phosphonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1148026-99-6
  • MF: C8H18BrO6P
  • MW: 321.103
  • Catalog: PROTAC Linker
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 458.1±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 230.9±31.5 °C

PROTAC Linker 9

PROTAC Linker 9 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 9 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: 206265-94-3
  • MF: C18H29NO7S
  • MW: 403.49000
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S,R,S)-AHPC-C7-amine

(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader[1].

  • CAS Number: 2306389-04-6
  • MF: C30H45N5O4S
  • MW: 571.77
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azidoethyl-PEG2-t-Butyl ester

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

  • CAS Number: 2144777-83-1
  • MF: C13H25N3O4S2
  • MW: 351.49
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG8-SH

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

  • CAS Number: 1422540-92-8
  • MF: C19H36O8S
  • MW: 424.55
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TNF-α-IN-1

TNF-α-IN-1 is a TNF-α inhibitor extracted from patent US20030096841A1, compound example I-7.

  • CAS Number: 444287-49-4
  • MF: C16H14ClN3O5
  • MW: 363.753
  • Catalog: Ligand for E3 Ligase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 718.6±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 388.4±32.9 °C

Tetrazine-Acid

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

  • CAS Number: 1380500-92-4
  • MF: C10H8N4O2
  • MW: 216.20
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TAMRA-PEG3-Azide

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

  • CAS Number: 1228100-59-1
  • MF: C33H38N6O7
  • MW: 646.733
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(m-PEG4)-N'-(DBCO-PEG4)-Cy5

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

  • CAS Number: 2107273-76-5
  • MF: C63H79ClN4O10
  • MW: 1087.78
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC BET degrader-2

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.

  • CAS Number: 2093388-33-9
  • MF: C41H42N10O6
  • MW: 770.84
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG5-OH

Propargyl-PEG5-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1036204-60-0
  • MF: C13H24O6
  • MW: 276.326
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 368.1±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 176.4±26.5 °C

Benzyl-PEG2-amine

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

  • CAS Number: 1268135-96-1
  • MF: C11H17NO2
  • MW: 195.258
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6-Maleimidocaproic acid sulfo-NHS

6-Maleimidocaproic acid sulfo-NHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 103848-61-9
  • MF: C14H16N2O9S
  • MW: 388.35000
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-Thalidomide

Biotin-Thalidomide is a cereblon affinity probe for PROTAC and targeted protein degradation research.

  • CAS Number: 2230857-87-9
  • MF: C44H64N8O13S
  • MW: 945.09
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4,7,10-TRIOXA-1,13-TRIDECANEDIAMINE

PROTAC Linker 24 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 24 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: 4246-51-9
  • MF: C10H24N2O3
  • MW: 220.309
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 310.6±0.0 °C at 760 mmHg
  • Melting Point: -32 °C
  • Flash Point: 148.0±17.4 °C

TCO-PEG3-acid

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

  • CAS Number: 2141981-86-2
  • MF: C18H31NO7
  • MW: 373.44
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-5-CH2-NH2 hydrochloride

Thalidomide-5-CH2-NH2 (hydrochloride) is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-CH2-NH2 (hydrochloride) can be connected to the ligand for protein by a linker to form PROTACs[1].

  • CAS Number: 1010100-22-7
  • MF: C14H14ClN3O4
  • MW: 323.73
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-NH-PEG7-acetic acid

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

  • CAS Number: 141282-29-3
  • MF: C21H41NO11
  • MW: 483.55
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-Acetyl-PEG3-C2-acid

S-Acetyl-PEG3-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1421933-33-6
  • MF: C11H20O6S
  • MW: 280.338
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 421.4±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 208.7±27.3 °C

(S,R,S)-AHPC-C6-NH2

PROTAC building block.

  • CAS Number: 2306389-03-5
  • MF: C29H43N5O4S
  • MW: 557.75
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-NH-PEG1-C2-NH2

Thalidomide-NH-PEG1-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: 2138439-12-8
  • MF: C17H20N4O5
  • MW: 360.365
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 660.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 353.3±31.5 °C

Thalidomide-4-NH-PEG1-NH-Boc

Thalidomide-4-NH-PEG1-NH-Boc is a Boc-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-4-NH-PEG1-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.

  • CAS Number: 2154342-17-1
  • MF: C22H28N4O7
  • MW: 460.48
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG3-phosphonic acid diethyl ester

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

  • CAS Number: 1148026-98-5
  • MF: C12H26BrO6P
  • MW: 377.209
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 426.5±35.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 211.7±25.9 °C

Azido-PEG3-S-PEG4-propargyl

Azido-PEG3-S-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055041-24-0
  • MF: C19H35N3O7S
  • MW: 449.56
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG6-thiol

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

  • CAS Number: 441771-60-4
  • MF: C13H28O6S
  • MW: 312.42300
  • Catalog: PROTAC Linker
  • Density: 1.057
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cbz-aminooxy-PEG8-acid

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

  • CAS Number: 2353410-09-8
  • MF: C27H45NO13
  • MW: 591.65
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG7-amine

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

  • CAS Number: 332941-25-0
  • MF: C16H36N2O7
  • MW: 368.46600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 40

E3 ligase Ligand-Linker Conjugates 40 incorporates a cIAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 40 can be used to design PROTAC degrader[1].

  • CAS Number: 2222354-20-1
  • MF: C39H56N4O11S
  • MW: 788.95
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CCT367766

CCT-367766 (CCT367766) is a novel heterobifunctional PROTAC that binds and degrades the putative transcription factor regulator Pirin in cells.

  • CAS Number: 2229856-58-8
  • MF: C49H48ClN7O11
  • MW: 946.41
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NHS-PEG4-SPDP

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

  • CAS Number: 1334177-95-5
  • MF: C23H33N3O9S2
  • MW: 559.653
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A