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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N-Boc-PEG8-alcohol

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

  • CAS Number: 1345337-22-5
  • MF: C21H43NO10
  • MW: 297.30376
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Alkynyl Palmitic Acid

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

  • CAS Number: 99208-90-9
  • MF: C16H28O2
  • MW: 252.392
  • Catalog: PROTAC Linker
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 371.8±15.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 180.7±15.1 °C

Aminooxy-PEG4-alcohol

Aminooxy-PEG4-alcohol is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Aminooxy-PEG4-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 106492-60-8
  • MF: C8H19NO5
  • MW: 209.24000
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG1-CH2CO2-NHS

Azido-PEG1-CH2CO2-NHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1480545-09-2
  • MF: C8H10N4O5
  • MW: 242.19
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-Hyp-OMe

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

  • CAS Number: 74844-91-0
  • MF: C11H19NO5
  • MW: 245.272
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 335.2±42.0 °C at 760 mmHg
  • Melting Point: 92-96 °C(lit.)
  • Flash Point: 156.6±27.9 °C

Mal-PEG6-Boc

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

  • CAS Number: 518044-37-6
  • MF: C23H39NO10
  • MW: 489.556
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 565.2±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 295.6±30.1 °C

t-Boc-Aminooxy-PEG3-amine

Boc-Aminooxy-PEG3-C2-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1235514-18-7
  • MF: C13H28N2O6
  • MW: 308.37
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-acid

Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells[1].

  • CAS Number: 1415800-32-6
  • MF: C12H20O6
  • MW: 260.284
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 388.0±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 141.0±20.0 °C

Ald-Ph-amido-PEG2-C2-Boc

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

  • CAS Number: 1807521-09-0
  • MF: C19H27NO6
  • MW: 365.421
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 547.6±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 285.0±28.7 °C

Methyltetrazine-PEG5-alkyne

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

  • CAS Number: 1802907-97-6
  • MF: C20H26N4O5
  • MW: 402.444
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 568.5±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 198.5±23.1 °C

Bromoacetamido-PEG5-DOTA

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

  • CAS Number: 2353410-19-0
  • MF: C30H55BrN6O13
  • MW: 787.69
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

endo-BCN-O-PNB

endo-BCN-O-PNB is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1263166-91-1
  • MF: C17H17NO5
  • MW: 315.32
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-C2-cyclohexylcarboxyl-hydrazide hydrochloride

Mal-C2-cyclohexylcarboxyl-hydrazide hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 174422-72-1
  • MF: C12H18ClN3O3
  • MW: 287.74
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S,R,S)-AHPC-C5-COOH

(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases[1].

  • CAS Number: 2267282-19-7
  • MF: C29H42N4O5S
  • MW: 558.73
  • Catalog: HIF/HIF Prolyl-Hydroxylase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH-bis(PEG2-Boc)

NH-bis(C2-PEG2-NH-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2182601-69-8
  • MF: C22H45N3O8
  • MW: 479.61
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH2-PEG2-C6-Cl

NH2-PEG2-C6-Cl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 744203-60-9
  • MF: C10H22ClNO2
  • MW: 223.74
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tos-PEG2-THP

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

  • CAS Number: 69502-32-5
  • MF: C16H24O6S
  • MW: 344.42
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG2-O-Ph-NH2

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

  • CAS Number: 65673-48-5
  • MF: C11H17NO3
  • MW: 211.25800
  • Catalog: PROTAC Linker
  • Density: 1.086g/cm3
  • Boiling Point: 346.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 173.9ºC

Diethylene Glycol Monobenzyl Ether

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

  • CAS Number: 2050-25-1
  • MF: C11H16O3
  • MW: 196.243
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 311.2±22.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 142.0±22.3 °C

DBCO-PEG4-NH-Boc

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

  • CAS Number: 2353410-17-8
  • MF: C34H45N3O8
  • MW: 623.74
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC BET Degrader-10

PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, with a DC50 of 49 nM[1].

  • CAS Number: 1957234-97-7
  • MF: C39H39ClN8O6S
  • MW: 783.29
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HEMTAC CDK4/6 degrader 1

HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1].

  • CAS Number: 2821803-61-4
  • MF: C48H53ClN16O4
  • MW: 953.49
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-Maleimidopropionic acid

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

  • CAS Number: 7423-55-4
  • MF: C7H7NO4
  • MW: 169.135
  • Catalog: PROTAC Linker
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 382.5±25.0 °C at 760 mmHg
  • Melting Point: 103-106 °C(lit.)
  • Flash Point: 185.1±23.2 °C

HS-PEG11-CH2CH2N3

HS-PEG11-CH2CH2N3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2148986-08-5
  • MF: C24H49N3O11S
  • MW: 587.72
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methyltetrazine-PEG24-amine

Methyltetrazine-PEG24-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2353410-18-9
  • MF: C57H105N5O24
  • MW: 1244.50
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dimethylamino-PEG2-C2-NH2

Dimethylamino-PEG2-C2-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 692782-62-0
  • MF: C8H20N2O2
  • MW: 176.26
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG5-2-methylacrylate

m-PEG5-2-methylacrylate is a PEG- and Alkyl/ester-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 48074-75-5
  • MF: C15H28O7
  • MW: 320.38
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cereblon inhibitor 1

Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research[1].

  • CAS Number: 2672489-14-2
  • MF: C32H28ClF2N5O4
  • MW: 620.05
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Azide-PEG3)-N'-(PEG4-acid)-Cy5

N-(Azide-PEG3)-N'-(PEG4-acid)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2107273-42-5
  • MF: C44H62ClN5O9
  • MW: 840.44
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HS-PEG8-CH2CH2COOH

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

  • CAS Number: 866889-02-3
  • MF: C19H38O10S
  • MW: 458.56400
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A