lenalidomide

Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.

Lenalidomide-Br (Compound 41), a derivative of Lenalidomide, acts as a ligand for cereblon (CRBN) - an E3 ubiquitin ligase involved in protein recruitment. This compound can be conjugated to a protein ligand via a linker to create PROTACs, such as the PROTAC STAT3 degrader SD-36.

Lenalidomide hemihydrate is a derivative of Thalidomide, an orally active immunomodulator that acts as a molecular gel. It is a ligand for the ubiquitin E3 ligase cereblon, which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase.

Lenalidomide-OH is an analog of Lenalidomide, a cereblon ligand for E3 ubiquitin ligase (CRBN), used for CRBN protein recruitment. It is able to attach to protein ligands using linkers to form PROTAC.

Lenalidomide-C5-amido-Boc is a Cereblon ligand derived from Lenalidomide, and serves in the recruitment of CRBN protein. It can be effectively linked to the protein ligand through a linker, resulting in the formation of PROTAC.

Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) is a Lenalidomide-based Cereblon ligand that facilitates CRBN protein recruitment and can be linked to the protein's ligand via a linker, forming a PROTAC[1].

Lenalidomide-6-F is a derivative of Lenalidomide that serves as a cereblon (CRBN) ligand facilitating the recruitment of CRBN protein. With the addition of a linker, Lenalidomide-6-F can be conjugated to the ligand for the protein, enabling the formation of PROTAC.

Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride serves as a specialized cerebellar ligand suitable for PROTAC development. It integrates an E3 ligand with a terminal piperidine, facilitating subsequent chemical reactions. This compound enables the creation of a protein degradant featuring a rigid connector [1].

Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs[1].

Functionalized cereblon ligand for PROTAC research and development; incorporates an E3 ligase ligand plus a PEG1 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

Lenalidomide-I (Compound 72) is a derivative of the cereblon (CRBN) ligand, Lenalidomide, with affinity for E3 ubiquitin ligase. It facilitates the recruitment of CRBN protein. Lenalidomide-I can be utilized in PROTACs, such as the PROTAC BET degrader QCA570, by linking it to the targeted protein ligand through a linker.

Lenalidomide (sodium), a Thalidomide derivative, serves as a molecular glue and an orally active immunomodulator. It acts as a cereblon (CRBN) ligand and triggers selective ubiquitination and subsequent degradation of the lymphoid transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 ubiquitin ligase. Echoing its specificity, Lenalidomide (sodium) inhibits the proliferation of mature B-cell lymphomas, notably multiple myeloma, and promotes IL-2 secretion from T cells [1] [2].

Lenalidomide 4'-alkyl-C5-azide, a functionalized cerebellar ligand designed for PROTAC development, comprises an E3 ligand and an alkyl LC5 ligand featuring terminal azides for coupling with a target protein ligand [1].

Lenalidomide-4-aminomethyl is a CRBN ligand derived from Lenalidomide, which is utilized for the recruitment of CRBN protein. By linking Lenalidomide-4-aminomethyl to the ligand, a PROTAC can be formed.

Lenalidomide-PEG3-iodine, an E3 ligase ligand-linker conjugate, consists of a cereblon-based Lenalidomide ligand and a 3-unit polyethylene glycol (PEG) linker. This compound is utilized in creating various proteolysis targeting chimeras (PROTACs), including the highly effective PROTAC BTK degrader SJF620, which has a degradation concentration 50 (DC50) of 7.9 nM[1].

Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride is a chemical compound comprising a cereblon (CRBN) ligand that functions as an E3 ubiquitin ligase, along with a linker. It is utilized to create the PROTAC MD-224[1].

Lenalidomide hydrochloride (CC-5013 hydrochloride), a Thalidomide derivative, functions as molecular glue and serves as an orally active immunomodulator. As a ligand for the ubiquitin E3 ligase cereblon (CRBN), it facilitates the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase. Specifically, Lenalidomide hydrochloride inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and promotes IL-2 release from T cells [1] [2].

Lenalidomide 5'-piperazine, a cerebellar ligand utilized in PROTAC development, facilitates the binding of an E3 ligand to its terminal piperazine. This connection enables subsequent chemical reactions aimed at generating a protein deactivator, employing a rigid linker [1].

Lenalidomide-C9-aldehyde is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a linker. Lenalidomide-C9-aldehyde can be used in the synthesis of a series of PROTACs, such as INY-03-041. INY-03-041

Lenalidomide-5-aminomethyl hydrochloride is a cereblon (CRBN) ligand derived from Lenalidomide. It serves as a ligand for the recruitment of the CRBN protein. When connected to the protein via a linker, Lenalidomide-5-aminomethyl hydrochloride forms a PROTAC.

Lenalidomide-5-Br is a Lenalidomide derivative that functions as a ligand for cereblon (CRBN), thereby facilitating the recruitment of CRBN protein. It can be conjugated to the protein ligand through a linker to generate a PROTAC molecule.

Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1].

Lenalidomide-4-aminomethyl hydrochloride is a compound derived from Lenalidomide, serving as a cereblon (CRBN) ligand for the recruitment of CRBN protein. By connecting Lenalidomide-4-aminomethyl hydrochloride to the ligand via a linker, PROTAC formation can be facilitated.

Lenalidomide-propargyl-C2-NH2 hydrochloride is a compound that features a cereblon (CRBN) ligand for the E3 ubiquitin ligase, as well as a linker. It is utilized in the development of the PROTAC MD-224[1] system.

Lenalidomide-C4-NH2 hydrochloride is a Cereblon ligand derived from Lenalidomide. It serves as a recruiting agent for the CRBN protein. The compound, known as PROTAC (Compound 24), can be formed by linking Lenalidomide-C4-NH2 hydrochloride to the ligand for the protein. It exhibits inhibitory effects with IC50s of 0.98 nM and 13.7 nM against the growth of RS4;11 and MOLM-13 acute leukemia cell lines, respectively[1].

Functionalized cereblon ligand for PROTAC research and development; incorporates an E3 ligase ligand plus a PEG2 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

Functionalized cereblon ligand for PROTAC research and development; incorporates an E3 ligase ligand plus a PEG3 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

Lenalidomide-4-OH is a cereblon (CRBN) ligand derived from Lenalidomide, utilized in the recruitment of the CRBN protein. It can be conjugated to the protein ligand via a linker, facilitating the formation of PROTAC.

Lenalidomide-C5-acid, a Lenalidomide-based E3 ligase ligand-linker conjugate, is utilized for the recruitment of CRBN protein and can be used to synthesize PROTACs [1].

Lenalidomide 4'-PEG2-azide, a Lenalidomide-derived Cereblon ligand, facilitates the recruitment of CRBN protein. This compound can be tethered via a linker to a protein ligand, enabling the formation of PROTAC [1].

Lenalidomide 4'-alkyl-C3-azide (compound 4a), a chemically modified version of the orally active immunomodulator lenalidomide, is engineered for the synthesis of PROTACs. This compound, serving as a ligand for the ubiquitin E3 ligase cereblon (CRBN), integrates an Azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with alkyne-bearing molecules. Additionally, it can undergo strain-promoted alkyne-azide cycloaddition reactions (SPAAC) with molecules containing DBCO or BCN groups [1].

9-Decyn-1-ol is an alkyl ether-based PROTAC linker used in synthesizing PROTACs, acting as a conjugation agent to combine GDC-0068 and Lenalidomide to form INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that inhibits Akt1, Akt2, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1].

Ipatasertib-NH2 dihydrochloride is a ligand for the target protein AKT in PROTAC [INY-03-041], comprising Ipatasertib-NH2, a ten-hydrocarbon linker, and the CRBN ligand Lenalidomide, which functions as an E3 ubiquitin ligase.

PROTAC ATR degrader-2 (Compound 8i) serves as a PROTAC degrader targeting ATR, effectively degrading it in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, with DC50 values of 22.9 and 34.5 nM, respectively. This compound induces apoptosis and inhibits the proliferation of AML cells. Additionally, PROTAC ATR degrader-2 demonstrates favorable pharmacokinetic properties and potent antitumor activity in a mouse model of AML. (Pink: ATR ligand; Blue: E3 ligase ligand Lenalidomide; Black: linker) [1]

INY-03-041 trihydrochloride, a potent and highly selective PROTAC-based pan-AKT degrader, comprises Ipatasertib, an ATP-competitive AKT inhibitor, conjugated to Lenalidomide. It effectively inhibits AKT1, AKT2, and AKT3 with IC50 values of 2.0, 6.8, and 3.5 nM, respectively [1].

PROTAC MLKL Degrader-1 (Compound 36) is a selective PROTAC degrader targeting MLKL, with a degradation maximum (D max) exceeding 90%. The compound incorporates modified cereblon (CRBN) ligands and a lenalidomide-linker within its structure, effectively inhibiting cell death in a TSZ-induced model of necroptosis.

Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for the target protein AKT used in PROTAC, binding to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 for AKT degradation[1].

INY-03-041, a potent and highly selective PROTAC-based pan-AKT degrader, inhibits AKT1, AKT2, and AKT3 with IC50s of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. This compound consists of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide.

Abd110 (compound 42i), a Lenalidomide-based PROTAC ATR kinase degrader, selectively reduces levels of ATR and phospho-ATR while not impacting the related kinases ATM and DNA-PKcs [1].

JET-209 is a potent proteolysis-targeting chimera (PROTAC) that effectively degrades CBP/p300, exhibiting half-maximal degradation concentration (DC50) values of 0.05 nM for CBP and 0.2 nM for p300. The compound comprises lenalidomide (the cereblon ligand), a connecting linker, and GNE-207 (the bromodomain inhibitor). JET-209 is utilized in cancer research [1].

SJF620 hydrochloride is a PROTAC that utilizes a lenalidomide analog to recruit CRBN and ligands to target Btk, exhibiting a DC50 of 7.9 nM [1].