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-PEGn-NHS ester

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

  • CAS Number: 174569-25-6
  • MF: (C2H4O)nC8H11NO5
  • MW: 1787.0688
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-Aminooxy-PEG2-azide

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

  • CAS Number: 252378-68-0
  • MF: C11H22N4O5
  • MW: 290.32
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG3-C6-Cl

Azido-PEG3-C6-Cl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1625717-44-3
  • MF: C12H24ClN3O3
  • MW: 293.79
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand 9

E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 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: 87304-15-2
  • MF: C21H32N2O6
  • MW: 408.48900
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ph-PEG3

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

  • CAS Number: 7204-16-2
  • MF: C12H18O4
  • MW: 226.26900
  • Catalog: PROTAC Linker
  • Density: 1.097g/cm3
  • Boiling Point: 351.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 166.6ºC

PROTAC HDAC6 degrader 1

PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines[1].

  • CAS Number: 2785404-76-2
  • MF: C37H46N6O10
  • MW: 734.80
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZ'6421

AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer[1].

  • CAS Number: 2361115-35-5
  • MF: C52H65F3N6O7S
  • MW: 975.17
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

OPSS-PEG8-COOH

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

  • CAS Number: 1334177-96-6
  • MF: C27H46N2O11S2
  • MW: 638.791
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 768.5±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 418.6±32.9 °C

Methyl 1-hydroxy-3,6,9,12-tetraoxapentadecan-15-oate

Hydroxy-PEG4-C2-methyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2228857-35-8
  • MF: C12H24O7
  • MW: 280.31
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pom-8PEG

Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader[1].

  • CAS Number: 2488761-03-9
  • MF: C29H43N3O12
  • MW: 625.66
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG13-Ms

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

  • CAS Number: 1059604-93-1
  • MF: C26H54O15S
  • MW: 638.76
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(m-PEG4)-N'-(Biotin-PEG2-amido-PEG4)-Cy5

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

  • CAS Number: 2107273-78-7
  • MF: C61H93ClN6O13S
  • MW: 1185.94
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ICG-Sulfo-OSu sodium

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

  • CAS Number: 190714-28-4
  • MF: C49H52N3NaO10S2
  • MW: 930.07
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S,R,S)-AHPC-PEG2-acid

(S,R,S)-AHPC-PEG2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2172820-09-4
  • MF: C30H42N4O8S
  • MW: 618.74
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tos-PEG1-CH2-Boc

Tos-PEG1-CH2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1643957-24-7
  • MF: C15H22O6S
  • MW: 330.397
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 449.0±30.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 225.4±24.6 °C

TCO-PEG2-amine

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

  • CAS Number: 2141981-87-3
  • MF: C15H28N2O4
  • MW: 300.39
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG4-methyl acetate

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

  • CAS Number: 77303-64-1
  • MF: C11H22O7
  • MW: 266.28800
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCO-OH

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

  • CAS Number: 85081-69-2
  • MF: C8H14O
  • MW: 126.19600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Deshydroxyethyl Dasatinib

Target Protein-binding moiety 8 is a compound binding to BCR-ABL, and used for inhibiting BCR-ABL activity.

  • CAS Number: 910297-51-7
  • MF: C20H22ClN7OS
  • MW: 443.95300
  • Catalog: PROTAC
  • Density: 1.404g/cm3
  • Boiling Point: N/A
  • Melting Point: >300ºC
  • Flash Point: N/A

2,3,5,6-Tetrafluorophenyl 1-(cyclooct-4-en-1-yloxy)-1-oxo-5,8,11,14,17,20,23,26-octaoxa-2-azanonacosan-29-oate

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

  • CAS Number: 2353410-06-5
  • MF: C34H51F4NO12
  • MW: 741.76
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG6-Boc

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

  • CAS Number: 361189-64-2
  • MF: C19H38O9
  • MW: 410.50000
  • Catalog: PROTAC Linker
  • Density: 1.068 g/ml
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

cIAP1 Ligand-Linker Conjugates 16

cIAP1 Ligand-Linker Conjugates 16 is an E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs.

  • CAS Number: 2143956-63-0
  • MF: C29H37N9O5S
  • MW: 623.73
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methyl acetate-PEG1-methyl acetate

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

  • CAS Number: 54665-51-9
  • MF: C8H14O6
  • MW: 206.19300
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sulfo DBCO-PEG4-amine

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

  • CAS Number: 2055198-05-3
  • MF: C32H46N4O10S
  • MW: 678.79
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC Sirt2 Degrader-1

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker and thalidomide, a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1].

  • CAS Number: 2098487-75-1
  • MF: C40H40N10O8S2
  • MW: 852.94
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TBMP

3-tert-Butyl-4-methoxyphenol is a PROTAC linker, belongs to alkyl/ether class, with insecticidal activity. 3-tert-Butyl-4-methoxyphenol also induced increased activities of glutathione (GSH) S-transferase and epoxide hydrolase in the liver and forestomach tissues of A/HeJ mice, regulating the carcinogen metabolism system[1][2].

  • CAS Number: 88-32-4
  • MF: C11H16O2
  • MW: 180.24
  • Catalog: Biochemical Assay Reagents
  • Density: 1.009 g/cm3
  • Boiling Point: 293.3ºC at 760 mmHg
  • Melting Point: 64℃
  • Flash Point: 136ºC

1H-Thieno[3,4-d]imidazole-4-pentanamide, hexahydro-N-[2-(2-hydroxyethoxy)ethyl]-2-oxo-, (3aS,4S,6aR)-

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

  • CAS Number: 717119-80-7
  • MF: C14H25N3O4S
  • MW: 331.43
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

M-PEG4-DBCO

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

  • CAS Number: 2228857-36-9
  • MF: C28H34N2O6
  • MW: 494.58
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide 4'-ether-alkylC2-amine

Thalidomide 4'-ether-alkylC2-amine 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: 390367-50-7
  • MF: C15H15N3O5
  • MW: 317.297
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 612.1±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 324.0±31.5 °C

TCO-PEG3-NHS ester

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

  • CAS Number: 2141981-88-4
  • MF: C22H34N2O9
  • MW: 470.51
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A