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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m-PEG4-CH2-acid

m-PEG4-CH2-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 874208-84-1
  • MF: C11H22O6
  • MW: 250.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ald-ph-peg2-t-butyl ester

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

  • CAS Number: 2100306-65-6
  • MF: C16H22O5
  • MW: 294.34
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lipoamido-PEG8-acid

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

  • CAS Number: 1334172-70-1
  • MF: C27H51NO11S2
  • MW: 629.824
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 748.3±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 406.4±32.9 °C

(S,R,S)-AHPC-O-Ph-PEG1-NH2

(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02 [1].

  • CAS Number: 2361117-24-8
  • MF: C32H41N5O6S
  • MW: 623.76
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG8-amine

Amino-PEG8-amine is a PEG-based (8 units) PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 82209-36-7
  • MF: C18H40N2O8
  • MW: 412.519
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 493.4±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 244.7±21.0 °C

DBCO-NH-(CH2)4COOH

DBCO-NH-(CH2)4COOH is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2375193-74-9
  • MF: C24H24N2O4
  • MW: 404.46
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-C2-amido-C2-COOH

Thalidomide-C2-amido-C2-COOH incorporates a CRBN ligand for the E3 ubiquitin ligase, and a linker. Thalidomide-C2-amido-C2-COOH can be used to design PROTAC CDK2/9 Degrader-1 (HY-130709)[1].

  • CAS Number: 2353496-84-9
  • MF: C19H20N4O7
  • MW: 416.38
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Carboxyrhodamine 110-PEG4-alkyne

Carboxyrhodamine 110-PEG4-alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055103-66-5
  • MF: C32H33N3O8
  • MW: 587.62
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cyclohexane-PEG1-Br

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

  • CAS Number: 131665-94-6
  • MF: C8H15BrO
  • MW: 207.10800
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S,R,S)-AHPC-C4-NH2

(S,R,S)-AHPC-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC[1].

  • CAS Number: 2138439-53-7
  • MF: C27H39N5O4S
  • MW: 529.69
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-Aminophenol-PEG4-methyl

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

  • CAS Number: 1429340-32-8
  • MF: C15H25NO5
  • MW: 299.36
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG1-NHS ester

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

  • CAS Number: 1807530-06-8
  • MF: C9H12N4O5
  • MW: 256.215
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG4-CH2COOH

Amino-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Amino-PEG4-CH2COOH is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 195071-49-9
  • MF: C10H21NO6
  • MW: 251.27700
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-Aminooxy-PEG11-amine

t-Boc-Aminooxy-PEG11-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1630094-83-5
  • MF: C29H60N2O14
  • MW: 660.79
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DNP-NH-PEG2-C2-acid

DNP-NH-PEG2-C2-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 1353011-89-8
  • MF: C13H17N3O8
  • MW: 343.289
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 573.7±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 300.8±30.1 °C

Propargyl-PEG5-CH2CO2-NHS

Propargyl-PEG4-O-C1-NHS ester (compound 8) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1161883-51-7
  • MF: C17H25NO9
  • MW: 387.38
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DBCO-PEG5-DBCO

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

  • CAS Number: 2363130-04-3
  • MF: C50H54N4O9
  • MW: 854.99
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG11-azide

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

  • CAS Number: 1392284-57-9
  • MF: C24H48N6O11
  • MW: 596.672
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ald-Ph-PEG2-NH-Boc

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

  • CAS Number: 1807503-90-7
  • MF: C19H28N2O6
  • MW: 380.435
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 581.3±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 305.4±30.1 °C

Benzyloxy carbonyl-PEG3-NHS ester

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

  • CAS Number: 2100306-68-9
  • MF: C21H27NO9
  • MW: 437.44
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DSPE-PEG8-Mal

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

  • CAS Number: 2112737-94-5
  • MF: C64H119N2O19P
  • MW: 1251.61
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BDP FL-PEG5-azide

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

  • CAS Number: 2093197-91-0
  • MF: C26H39BF2N6O6
  • MW: 580.43
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Folate-PEG3-azide

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

  • CAS Number: 1313026-32-2
  • MF: C27H35N11O8
  • MW: 641.64
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 5 Free Base

E3 ligase Ligand-Linker Conjugates 5 Free Base is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 2010159-56-3
  • MF: C30H45N5O7S
  • MW: 619.77
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand 8

E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].

  • CAS Number: 1225383-33-4
  • MF: C31H34N2O6
  • MW: 530.61
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

endo-BCN-PEG2-acid

endo-BCN-PEG2-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1993134-72-7
  • MF: C18H27NO6
  • MW: 353.41
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propynol Ethoxylate

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

  • CAS Number: 3973-18-0
  • MF: C5H8O2
  • MW: 100.116
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 168.7±15.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 68.9±14.6 °C

N-methyl-N'-(propargyl-PEG4)-Cy5 (chloride)

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

  • CAS Number: 2107273-04-9
  • MF: C37H47ClN2O4
  • MW: 619.23
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG17-acid

Bis-PEG17-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2226897-74-9
  • MF: C38H74O21
  • MW: 866.98
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ac4ManNAz

Ac4ManNAz is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 361154-30-5
  • MF: C16H22N4O10
  • MW: 430.37
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A