Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2), 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].

Thalidomide-O-amido-C8-NH2 is a degron-linker (refer to Compound DL7-TL). The PROTAC linker is bound lo at least one targeting ligand. Degron-linker-targeting ligand, wherein the linker is covalently bound lo at least one degron and at least one targeting ligand, the degron is a compound capable of binding to an ubiquitin ligase such as an E3 ubiquitin ligase (e g, cereblon), and the targeting ligand is capable of binding to the targeted protein (s)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

458.51

C₂₃H₃₀N₄O₆

1950635-15-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. James Bradner, et al. Methods to induce targeted protein degradation through bifunctional molecules. WO 2017024317 A2.

cIAP1 Ligand-Linker Conjugates 2 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 2 can be used to design SNIPERs^[1].

660.80

C₃₇H₄₈N₄O₇

1312302-14-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorg Med Chem. 2011 Nov 15;19(22):6768-78.

cIAP1 Ligand-Linker Conjugates 3 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 3 can be used to design SNIPERs^[1].

788.95

C₃₉H₅₆N₄O₁₁S

2222354-20-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Heterocyclic compound. WO2018066545A1.

cIAP1 Ligand-Linker Conjugates 1 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 1 can be used to design SNIPERs^[1].

798.00

C₄₁H₅₉N₅O₉S

2357114-75-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nello Mainolfi, et al. Irak degraders and uses thereof. US20190192668A1.

VHL Ligand-Linker Conjugates 15 incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs^[1].

724.84

C₃₇H₄₅FN₄O₈S

2375564-62-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Farnaby W, et al. BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design. Nat Chem Biol. 2019 Jul;15(7):672-680.

Pomalidomide-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 22) 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].

Pomalidomide-amido-PEG3-C2-NH2 (Compound 5b) can be used to synthesize BI-3663. BI-3663 (cereblon-based) degrades focal adhesion tyrosine kinase (PTK2) with a median DC₅₀ of 30 nM to >80% across a panel of 11 human hepatocellular carcinoma (HCC) cell lines^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

476.48

C₂₂H₂₈N₄O₈

2328070-52-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520.

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].

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

430.45

C₂₁H₂₆N₄O₆

1950635-13-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Bradner J, et al. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses. WO 2017024318 A1.

cIAP1 Ligand-Linker Conjugates 5 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 5 can be used to design SNIPERs^[1].

729.93

C₃₇H₅₅N₅O₈S

2113688-20-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Shibata N, et al. Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands. J Med Chem. 2018 Jan 25;61(2):543-575.

AhR Ligand-Linker Conjugates 1 (E3 Ligase Ligand-Linker Conjugates 57) incorporates an IAP ligand for the E3 ubiquitin ligase, and a SNIPER linker. AhR Ligand-Linker Conjugates 1 can be used to design SNIPER^[1].

433.50

C₂₆H₂₇NO₅

2380012-98-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ohoka N, et al. Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins. ACS Chem Biol. 2019 Oct 16.

cIAP1 Ligand-Linker Conjugates 15 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 hydrochloride can be used to design SNIPERs^[1].

698.25

C₃₇H₄₈ClN₃O₈

1225383-36-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins. J Am Chem Soc. 2010 Apr 28;132(16):5820-6.

cIAP1 Ligand-Linker Conjugates 11 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 can be used to design SNIPERs^[1].

617.73

C₃₅H₄₃N₃O₇

1239943-19-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins. J Am Chem Soc. 2010 Apr 28;132(16):5820-6.

cIAP1 Ligand-Linker Conjugates 12 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 12 can be used to design SNIPERs^[1].

929.15

C₄₆H₆₄N₄O₁₂S₂

2095244-52-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ohoka N, et al. In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs). J Biol Chem. 2017 Mar 17;292(11):4556-4570.

cIAP1 Ligand-Linker Conjugates 14 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 14 can be used to design SNIPERs^[1].

719.82

C₃₉H₄₉N₃O₁₀

1351169-40-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorg Med Chem. 2011 Nov 15;19(22):6768-78.

cIAP1 Ligand-Linker Conjugates 11 Hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 Hydrochloride can be used to design SNIPERs^[1].

654.19

C₃₅H₄₄ClN₃O₇

1239866-59-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins. J Am Chem Soc. 2010 Apr 28;132(16):5820-6.

cIAP1 Ligand-Linker Conjugates 15 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 can be used to design SNIPERs^[1].

661.78

C₃₇H₄₇N₃O₈

1225433-96-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins. J Am Chem Soc. 2010 Apr 28;132(16):5820-6.

Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is composed of Degron (E3 ubiquitin ligase) and a linker, and they are used in PROTAC technology. Thalidomide-O-amido-PEG3-C2-NH2 binds to the targeting ligand to induce the target protein (including BRD4, BRD2, and BRD3) degradation^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

506.51

C₂₃H₃₀N₄O₉

1957236-20-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Methods to induce targeted protein degradation through bifunctional molecules. WO 2017007612 A1

Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6), 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].

Thalidomide-O-amido-C4-NH2 is an amine intermediate (Compound 41), which can be used as is a heterobifunctional PROTAC BET degrader. The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases. Recently, heterobifunctional small-molecule BET degraders have been designed based upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation^[1]. Thalidomide-O-amido-C4-NH2 is a degron-linker (refer to Compound DL6-TL). Degron-linker-targeting ligand, wherein the linker is covalently bound lo at least one degron and at least one targeting ligand, the degron is a compound capable of binding to an ubiquitin ligase such as an E3 ubiquitin ligase (e g, cereblon), and the targeting ligand is capable of binding to the targeted protein (s)^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

402.40

C₁₉H₂₂N₄O₆

1799711-24-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins withPicomolar Cellular Potencies and Capable of Achieving Tumor Regression.J Med Chem. 2018 Jan 25;61(2):462-481.

  [2]. James Bradner, et al. Methods to induce targeted protein degradation through bifunctional molecules. WO 2017024317 A2.

cIAP1 Ligand-Linker Conjugates 4 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 4 can be used to design SNIPERs^[1].

974.15

C₅₅H₆₇N₅O₁₁

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorg Med Chem. 2011 Nov 15;19(22):6768-78.

cIAP1 Ligand-Linker Conjugates 4 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 4 can be used to design SNIPERs^[1].

974.15

C₅₅H₆₇N₅O₁₁

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorg Med Chem. 2011 Nov 15;19(22):6768-78.

cIAP1 Ligand-Linker Conjugates 4 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 4 can be used to design SNIPERs^[1].

974.15

C₅₅H₆₇N₅O₁₁

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Itoh Y, et al. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorg Med Chem. 2011 Nov 15;19(22):6768-78.