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-(Amino-PEG5)-N-bis(PEG4-acid)

N-(Amino-PEG5)-N-bis(PEG4-acid) is a PEG-based PROTAC linker used in the synthesis of PROTACs. N-(Amino-PEG5)-N-bis(PEG4-acid) contains an amino group with two terminal carboxylic acids[1].

  • CAS Number: 2093152-86-2
  • MF: C34H68N2O17
  • MW: 776.91
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

endo-BCN-PEG2-NH2

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

  • CAS Number: 1263166-93-3
  • MF: C17H28N2O4
  • MW: 324.41500
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-PEG4-COOH

Pomalidomide-PEG4-COOH is a E3 ligase ligand-linker conjugate. Pomalidomide-PEG4-COOH contains the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology (extracted from patent WO2017184995A1)[1].

  • CAS Number: 2138440-81-8
  • MF: C24H31N3O10
  • MW: 521.517
  • Catalog: Ligand for E3 Ligase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 773.6±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 421.6±32.9 °C

Azido-PEG4-CH2-Boc

Azido-PEG4-CH2-Boc is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Azido-PEG4-CH2-Boc is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[2].

  • CAS Number: 864681-04-9
  • MF: C14H27N3O6
  • MW: 333.38100
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HO-PEG17-OH

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

  • CAS Number: 351342-04-6
  • MF: C34H70O18
  • MW: 766.91
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG3-bromide

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

  • CAS Number: 203740-63-0
  • MF: C9H15BrO3
  • MW: 251.118
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 287.8±25.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 115.0±21.7 °C

Thalidomide-O-amido-C6-NH2

Thalidomide-O-amido-C6-NH2 (Cereblon Ligand-Linker Conjugates 11), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].

  • CAS Number: 1950635-13-8
  • MF: C21H26N4O6
  • MW: 430.45
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-PEG3-amide-CH2OCH2COOH

Fmoc-NH-PEG3-amide-CH2OCH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 489427-26-1
  • MF: C27H34N2O9
  • MW: 530.56700
  • Catalog: PROTAC Linker
  • Density: 1.256g/cm3
  • Boiling Point: 794.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 434.5ºC

1-(4-(6-Methyl-1,2,4,5-tetrazin-3-yl)phenoxy)-3,6,9,12-tetraoxapentadecan-15-oic acid

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

  • CAS Number: 1802907-91-0
  • MF: C20H28N4O7
  • MW: 436.459
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 647.6±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 345.5±34.3 °C

Ac4GalNAl

Ac4GalNAl is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1673590-09-4
  • MF: C19H25NO10
  • MW: 427.40
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-NH-(CH2)3-NH-Boc

Thalidomide-NH-(CH2)3-NH-Boc is a Boc-modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)3-NH-Boc is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules targeting 11β-substituted estradiol.

  • CAS Number: 2093386-36-6
  • MF: C21H26N4O6
  • MW: 430.45
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FC-11

FC-11 is a PROTAC FAK degrader (DC90: 1 nM) . FC-11 contains CRBN ligand Pomalidomide (HY-10984), linker and FAK ligand PF562271 (HY-10459). FC-11 degrades FAK in various cells, with DC50s of 310 pM in TM3, 80 pM in PA1, 330 pM in MDA-MB-436, 370 pM in LNCaP, and 40 pM in Ramos cells[1].

  • CAS Number: 2271035-37-9
  • MF: C41H42F3N13O9S
  • MW: 949.91
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG2-NHS ester

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

  • CAS Number: 2512228-06-5
  • MF: C12H15NO6
  • MW: 269.25
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Azido-PEG4-N-Boc-N-PEG3-Boc

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

  • CAS Number: 2093152-85-1
  • MF: C28H54N4O11
  • MW: 622.75
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BnO-PEG1-CH2COOH

BnO-PEG1-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 93206-09-8
  • MF: C11H14O4
  • MW: 210.22600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Triethylene glycol monododecyl ether

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

  • CAS Number: 3055-94-5
  • MF: C18H38O4
  • MW: 318.492
  • Catalog: PROTAC Linker
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 412.0±25.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 202.9±23.2 °C

N-(Boc-PEG1)-N-bis(PEG2-propargyl)

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

  • CAS Number: 2100306-63-4
  • MF: C23H40N2O7
  • MW: 456.57
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG3-C3-NH2

Biotin-PEG3-C3-NH2 is a PEG-based PROTAC linker, with NH2 functional group, that can be used in the synthesis of PROTACs[1].

  • CAS Number: 183896-00-6
  • MF: C20H38N4O5S
  • MW: 446.60
  • Catalog: PROTAC Linker
  • Density: 1.139±0.06 g/cm3(Predicted)
  • Boiling Point: 715.3±60.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-PEG3-azide

Pomalidomide-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology[1].

  • CAS Number: 2267306-15-8
  • MF: C21H24N6O8
  • MW: 488.45
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 Ligase Ligand-Linker Conjugates 25 Trifluoroacetate

E3 Ligase Ligand-Linker Conjugates 25 Trifluoroacetate is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 1950635-14-9
  • MF: C23H27F3N4O8
  • MW: 544.48
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nonylbenzene-PEG5-OH

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

  • CAS Number: 20636-48-0
  • MF: C25H44O6
  • MW: 440.61300
  • Catalog: PROTAC Linker
  • Density: 1.016g/cm3
  • Boiling Point: 541.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 281.1ºC

Benzyl-PEG1-Ms

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

  • CAS Number: 58841-52-4
  • MF: C10H16O5S
  • MW: 248.29600
  • Catalog: PROTAC Linker
  • Density: 1.218g/cm3
  • Boiling Point: 375.438ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 180.858ºC

H2n-peg14-oh

Amino-PEG14-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 34214-89-6
  • MF: C28H59NO14
  • MW: 633.77
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 Ligase Ligand-Linker Conjugates 24 TFA

E3 Ligase Ligand-Linker Conjugates 24 (TFA) incorporates an E3 ligase ligand and a linker, can be an immunomodulater for the treatment of cancer.

  • CAS Number: 1957235-75-4
  • MF: C23H27F3N4O10
  • MW: 576.48
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-C3-NH2 hydrochloride

Pomalidomide-C3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 2154342-45-5
  • MF: C16H19ClN4O4
  • MW: 366.80
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methyltetrazine-PEG5-NHS ester

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

  • CAS Number: 1802907-92-1
  • MF: C24H31N5O9
  • MW: 533.53
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG10-acid

Azido-PEG10-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG2-C4-alkyne

Biotin-PEG2-C4-alkyne is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1011268-28-2
  • MF: C22H36N4O5S
  • MW: 468.610
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 799.8±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 437.5±32.9 °C

Methyl azetidine-3-carboxylate hydrochloride

Methyl azetidine-3-carboxylate hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Methyl azetidine-3-carboxylate hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs<

  • CAS Number: 100202-39-9
  • MF: C5H10ClNO2
  • MW: 151.591
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: 190.9ºC at 760 mmHg
  • Melting Point: 93.0 to 97.0 °C
  • Flash Point: 69.3ºC

CD147 degrader 1

CD147 degrader 1 is a PROTAC targets CD147 with an DC50 value of 6.72 µM. CD147 degrader 1 inhibits cell proliferation, migration and invasion. CD147 degrader 1 decreases the expression of CD147, MMP9, and p-STAT3 protein. CD147 degrader 1 shows anti-cancer acyivity[1].

  • CAS Number: 2416740-37-7
  • MF: C38H42N4O11
  • MW: 730.76
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A