Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1642 |
Lenalidomide
来那度胺,CC-5013 |
Apoptosis; TNF; Ligand for E3 Ligase; Molecular Glues | Apoptosis; PROTAC |
Lenalidomide (CC-5013) 是 Thalidomide 的衍生物,也是具有口服活性免疫调节剂,以分子胶的方式作用。它是泛素 E3 连接酶 cereblon (CRBN) 的配体,可通过 CRBN-CRL4 泛素连接酶对两种淋巴转录因子 IKZF1 和 IKZF3 进行选择性泛素化和降解。 | |||
T18066 |
Lenalidomide-OH
|
Ligand for E3 Ligase | PROTAC |
Lenalidomide-OH是cereblon (CRBN)的配体,作为E3泛素连接酶的Lenalidomide类似物。它用于CRBN蛋白的招募。此外,通过连接器,Lenalidomide-OH可以与蛋白质配体结合,形成PROTACs。一个包含Lenalidomide-OH的PROTAC BTK降解剂的例子是SJF620。 | |||
T9270 |
C5 Lenalidomide
来那度胺杂质13 |
Others | Others |
C5 Lenalidomide 是一种具有不确定生物活性的化学物质。 | |||
T18064 |
Lenalidomide-Br
|
Ligand for E3 Ligase | PROTAC |
Lenalidomide-Br是Lenalidomide的衍生物,作为cereblon (CRBN)的配体,后者是参与蛋白质招募的E3泛素连接酶。通过连接器,Lenalidomide-Br可与蛋白质配体偶联,构建PROTACs。例如,Lenalidomide-Br被作为PROTAC STAT3降解剂SD-36的组成部分利用。 | |||
T22922 |
Lenalidomide hemihydrate
|
TNF; Ligand for E3 Ligase; Molecular Glues | Apoptosis; PROTAC |
Lenalidomide hemihydrate 是 Thalidomide 的衍生物,也是具有口服活性免疫调节剂,以分子胶的方式作用。它是泛素 E3 连接酶 cereblon 的配体,通过 CRBN-CRL4 泛素连接酶对两种淋巴转录因子 IKZF1 和 IKZF3 进行选择性泛素化和降解。 | |||
T36257 |
Lenalidomide 4'-PEG1-amine
Lenalidomide 4'-PEG1-amine |
||
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. | |||
T39599 |
Lenalidomide-C5-amido-Boc
Lenalidomide-C5-amido-Boc |
||
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. | |||
T36259 |
Lenalidomide 4'-PEG3-amine
Lenalidomide 4'-PEG3-amine |
||
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. | |||
T36258 |
Lenalidomide 4'-PEG2-amine
Lenalidomide 4'-PEG2-amine |
||
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. | |||
T39679 | Lenalidomide-I | ||
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. | |||
T40129 | Lenalidomide-6-F | ||
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. | |||
T38457 |
Lenalidomide-4-OH
|
||
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. | |||
T40897 |
Lenalidomide-4-aminomethyl
|
||
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. | |||
T38409 |
Lenalidomide-5-Br
|
||
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. | |||
T21763 | Lenalidomide hydrochloride | ||
Lenalidomide hydrochloride (CC-5013 hydrochloride) 是 Thalidomide 的衍生物,也是一种具有口服活性免疫调节剂,以分子胶的方式作用。Lenalidomide hydrochloride (CC-5013 hydrochloride) 是一种泛素 E3 连接酶 cereblon (CRBN) 的配体,通过 CRBN-CRL4 泛素连接酶对两种淋巴转录因子 IKZF1 和 IKZF3 进行选择性泛素化和降解。Lenalidomide hydrochloride (CC-5013 hydrochloride) 特异性抑制成熟 B 细胞淋巴瘤 (包括多发性骨髓瘤) 的生长,并诱导 T 细胞释放白细胞介素-2 (IL-2)。 | |||
T38545 | Lenalidomide-5-aminomethyl hydrochloride | ||
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. | |||
T40547 |
Lenalidomide-4-aminomethyl hydrochloride
|
||
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. | |||
T18068 |
Lenalidomide-PEG3-iodine
|
Others | Others |
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]. | |||
T18067 |
Lenalidomide-PEG1-azide
|
Others | Others |
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]. | |||
T18065 |
Lenalidomide-C9-aldehyde
|
Others | Others |
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 | |||
T18063 |
Lenalidomide-acetylene-C5-COOH
Cereblon ligand-linker Conjugate |
Others | Others |
Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) serves as a Lenalidomide-based Cereblon ligand that facilitates the recruitment of the CRBN protein. This compound can be connected to the protein's ligand through a linker, resulting in the formation of PROTAC[1]. | |||
T17928 |
Lenalidomide-C5-NH2
E3 ligase Ligand-Linker Conjugates 31,Cereblon Ligand-Linker Conjugates 19 |
Others | Others |
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]. | |||
T18070 |
Lenalidomide-propargyl-C2-NH2 hydrochloride
|
Others | Others |
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. | |||
T17878 |
Lenalidomide-C4-NH2 hydrochloride
Cereblon ligand 1 hydrochloride,E3 ligase Ligand-Linker Conjugates 32 hydrochloride |
Others | Others |
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]. | |||
T81942 |
Lenalidomide sodium
CC-5013 sodium |
||
Lenalidomide (sodium)是Thalidomide的衍生物,这种口服活性的免疫调节剂通过分子胶模式作用。作为泛素E3连接酶cereblon(CRBN)的配体,Lenalidomide (sodium)通过CRBN-CRL4泛素连接酶复合体,针对淋巴转录因子IKZF1和IKZF3进行选择性泛素化和降解。此外,Lenalidomide (sodium)有效抑制成熟B细胞淋巴瘤的增长,如多发性骨髓瘤,并能促使T细胞分泌白细胞介素-2(IL-2)。 | |||
T18069 |
Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride
|
Others | Others |
Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride is a chemical compound that features a cereblon (CRBN) ligand, functioning as an E3 ubiquitin ligase, along with a linker. It can be utilized to create the PROTAC MD-224[1]. | |||
T35386 |
Elotuzumab
Elotuzumab (anti-SLAMF7),BMS 901608,PDL 063,HuLuc 63 |
Others | Others |
Elotuzumab(HuLuc 63) (anti-SLAMF7) 是一种靶向 SLAMF7 受体的单克隆抗体。Elotuzumab (anti-SLAMF7) 是一种直接激活NK细胞并诱导抗体依赖性细胞毒性的化合物,可联合来那度胺和地塞米松 (Ld) 用于治疗多发性骨髓瘤。 | |||
T74002 | SJF620 hydrochloride | PROTACs | PROTAC |
SJF620 hydrochloride,作为一种连接Cereblon配体和Btk配体的PROTAC,具备DC50值为7.9 nM。该化合物含Lenalidomide类似物,能有效募集CRBN。 | |||
T79831 |
PROTAC MLKL Degrader-1
|
||
PROTACMLKL Degrader-1 (Compound 36) 为MLKL的PROTAC靶向降解剂,具有超过90%的Dmax效率。该化合物构成包含了修饰后的CRBN配体、linker 及 Lenalidomide 接头片段,能有效消除TSZ坏死模型中的细胞死亡。 | |||
T11664 |
INY-03-041
|
Others | Others |
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. | |||
T38393 |
Ipatasertib-NH2 dihydrochloride
RG7440-NH2 dihydrochloride,Ipatasertib-NH2 dihydrochloride,GDC-0068-NH2 dihydrochloride |
||
Ipatasertib-NH2 dihydrochloride is a ligand for the target protein AKT in PROTAC INY-03-041. INY-03-041 consists of Ipatasertib-NH2, a ten-hydrocarbon linker, and the CRBN ligand Lenalidomide, which acts as an E3 ubiquitin ligase. | |||
T60478 |
BTX161
|
||
BTX161 是沙利度胺类似物。BTX161是有效的 CKIα降解剂。在人类 AML 细胞中,BTX161 比来那度胺更好地介导 CKIα 降解,激活 DNA 损伤反应 (DDR) 和 p53,并能稳定 p53 拮抗剂 MDM2。 | |||
T18053 |
Ipatasertib-NH2
RG7440-NH2,GDC-0068-NH2 |
Others | Others |
Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC, binds to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 to degrade AKT[1]. | |||
T79230 |
JET-209
|
PROTACs | PROTAC |
JET-209为高效PROTAC CBP/p300降解剂,DC50分别为CBP和p300的0.05 nM与0.2 nM。该化合物融合了Lenalidomide (cereblon配体)、连接子以及GNE-207 (溴结构域抑制剂)。JET-209主要应用于癌症研究领域。 | |||
T74001 | INY-03-041 trihydrochloride | ||
INY-03-041 trihydrochloride 是一种有效的、高选择性的、基于PROTAC 的泛-AKT 降解剂,由ATP 竞争性AKT 抑制剂Ipatasertib 结合Lenalidomide 组成。INY-03-041 trihydrochloride 可抑制AKT1,AKT2和AKT3,IC50分别为 2.0 nM,6.8 nM 和 3.5 nM。 | |||
T18680 |
SD-36
|
Others | Others |
SD-36, a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), exhibits high specificity for STAT3 over other STAT members. It effectively targets both wild-type and mutated STAT3 proteins in cells, inhibiting their transcriptional activity (IC50=10 nM). The compound, consisting of the STAT3 inhibitor SI-109, a linker, and a CRBN ligand Lenalidomide analog for E3 ubiquitin ligase[1], demonstrates significant anti-tumor effects and achieves complete, long-lasting tumor regression in mouse mod... | |||
T17346 | 9-Decyn-1-ol | Others | Others |
9-Decyn-1-ol is an alkyl/ether-based PROTAC linker suitable for synthesizing PROTACs. It serves as a conjugation agent to combine GDC-0068 and Lenalidomide, resulting in the formation of INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that operates through the PROTAC mechanism. It effectively inhibits Akt1, Akt2, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1]. | |||
T36429 |
Dihydrodiol-Ibrutinib
|
||
PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A. 1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015) |