Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T39727 |
ERα degrader-2
|
ERK | MAPK |
ERα degrader-2 是一种具有选择性和有效性的雌激素受体 (SERD)降解剂,具有抗癌活性,抑制 ERα,对雌激素受体降解的 EC50 值为 0.3 nM。ERα degrader-2 可用于预防和治疗 HER 阳性乳腺癌。 | |||
T13721 |
Homo-PROTAC cereblon degrader 1
|
Others; PROTACs | Others; PROTAC |
Homo-PROTAC cereblon degrader 1 (compound 15a) 是一种高效 cereblon 降解剂,对 IKZF1 和 IKZF3 的影响很小。 | |||
T13722 |
Homo-PROTAC pVHL30 degrader 1
|
Others; PROTACs | Others; PROTAC |
Homo-PROTAC pVHL30 degrader 1 是一种基于 PROTAC 的 pVHL30 降解剂。 | |||
T9236 |
WSB1 Degrader 1
|
Others; E1/E2/E3 Enzyme | Others; Ubiquitination |
WSB1 Degrader 1 是具有口服活性的 WSB1降解剂,具有抗癌活性。 | |||
T69753 |
HDAC6 degrader 9c
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC6 degrader 9c 是一种小分子组蛋白脱乙酰酶 6 (HDAC6) 降解剂,可用于研究癌症或其他疾病。 | |||
T4207 |
(S,R,S)-AHPC hydrochloride
VHL Ligand 1 hydrochloride,ULM-1,Protein degrader 1 hydrochloride |
Others; Ligand for E3 Ligase | Others; PROTAC |
(S,R,S)-AHPC hydrochloride (Protein degrader 1 hydrochloride) 是基于 VH032 的 VHL 配体,可用于募集 von Hippel-Lindau (VHL) 蛋白。它能够利用 linker 与靶蛋白配体连接,得到 PROTAC 分子。 | |||
T40112 |
PROTAC PD-1/PD-L1 degrader-1
|
PD-1/PD-L1; PROTACs | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation; PROTAC |
PROTAC PD-1/PD-L1 degrader-1 是一种降解 PD-L1 的 PROTAC,抑制 PD-1/PD-L1 相互作用(IC50:39.2 nM)。PROTAC PD-1/PD-L1 degrader-1 可恢复 Hep3B/OS-8/hPD-L1 和 CD3 T 细胞共培养模型中被抑制的免疫力,可通过溶酶体依赖性方式降低 PD-L1 的蛋白质含量。 | |||
T37329 |
PROTAC IDO1 Degrader-1
PROTAC IDO1 Degrader-1 |
PROTACs | PROTAC |
PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1]. PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24... | |||
T40072 |
PROTAC BRD4 Degrader-9
PROTAC BRD4 Degrader-9 |
Others | Others |
PROTAC BRD4 Degrader-9 (compound 8a) is a novel chemical compound consisting of ligands for von Hippel-Lindau and BRD4, connected by a PROTAC moiety. This compound can effectively degrade the BRD4 protein in PC3 prostate cancer cells. When conjugated with STEAP1 and CLL1 antibodies, PROTAC BRD4 Degrader-9 exhibits potent activity, with respective DC50 values of 0.86 nM and 7.6 nM. | |||
T39902 |
PROTAC IRAK4 degrader-5
PROTAC IRAK4 degrader-5 |
Others | Others |
PROTAC IRAK4 degrader-5 is a Cereblon-based IRAK4 degrader. | |||
T36242 |
PROTAC BRD4 Degrader-5
PROTAC BRD4 Degrader-5 |
PROTACs | PROTAC |
PROTAC BRD4 Degrader-5 is a PROTAC-based BRD4 degrader. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines[1]. | |||
T40073 |
PROTAC BRD4 Degrader-10
PROTAC BRD4 Degrader-10 |
PROTACs | PROTAC |
PROTAC BRD4 Degrader-10, also known as compound 8b, is a dual ligand-based PROTAC that combines ligands for von Hippel-Lindau and BRD4. To degrade the BRD4 protein in PC3 prostate cancer cells, PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies, with respective DC 50 values of 1.3 nM and 18 nM. | |||
T40074 |
PROTAC BRD4 Degrader-15
PROTAC BRD4 Degrader-15 |
Others | Others |
PROTAC BRD4 Degrader-15 is a chemical compound consisting of a PROteolysis TArgeting Chimera (PROTAC) linked to ligands specific to von Hippel-Lindau and BRD4. It exhibits an IC50 of 7.2 nM for BRD4 BD1 and 8.1 nM for BRD4 BD2. Additionally, PROTAC BRD4 Degrader-15 demonstrates potent degradation activity against the BRD4 protein in PC3 prostate cancer cells. | |||
T40143 |
PROTAC CBP/P300 Degrader-1
PROTAC CBP/P300 Degrader-1 |
PROTACs | PROTAC |
PROTAC CBP/P300 Degrader-1 is an effective compound that degrades CBP/P300 in a potent manner. It significantly reduces cell viability in various cancer cell lines. | |||
T39920 |
PROTAC IRAK4 degrader-3
PROTAC IRAK4 degrader-3 |
PROTACs | PROTAC |
PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau. | |||
T36628 |
PROTAC BRD4 Degrader-8
PROTAC BRD4 Degrader-8 |
PROTACs | PROTAC |
PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degra... | |||
T39903 |
PROTAC IRAK4 degrader-6
PROTAC IRAK4 degrader-6 |
Others | Others |
PROTAC IRAK4 degrader-6 is a potent Cereblon-based compound designed to degrade interleukin-1 receptor-associated kinase 4 (IRAK4). | |||
T39901 |
PROTAC IRAK4 degrader-4
PROTAC IRAK4 degrader-4 |
Others | Others |
PROTAC IRAK4 degrader-4 (US20190192668A1, compound I-127) is a Cereblon-based PROTAC specifically designed to target and degrade interleukin-1 receptor-associated kinase 4 (IRAK4). | |||
T40250 |
SHP2 protein degrader-1
SHP2 protein degrader-1 |
Others | Others |
SHP2 protein degrader-1 is a highly efficient allosteric inhibitor targeting SHP2. It effectively induces degradation of SHP2 protein, resulting in cell apoptosis. This compound shows promising potential for studying diseases associated with SHP2. | |||
T39996 |
PROTAC CDK9 degrader-4
PROTAC CDK9 degrader-4 |
Others | Others |
PROTAC CDK9 degrader-4 is a potent and efficacious chemical compound designed specifically to degrade CDK9, a protein involved in transcription regulation. This compound effectively targets and reduces the levels of CDK9, thereby modulating transcriptional activity. | |||
T40075 |
PROTAC BRD4 Degrader-13
PROTAC BRD4 Degrader-13 |
Others | Others |
PROTAC BRD4 Degrader-13 (compound 9d) is a bioactive compound that functions as a proteolysis targeting chimera (PROTAC), linking ligands for von Hippel-Lindau and BRD4 proteins. In the context of PC3 prostate cancer cells, this compound effectively degrades the BRD4 protein through conjugation with STEAP1 and CLL1 antibodies. The degradation of BRD4 protein is achieved with remarkable potency, exhibiting a DC 50 of 0.025 nM and 6.0 nM when combined with STEAP1 and CLL1 antibodies, respectively. | |||
T77518 |
BLK degrader 1
|
Others | Others |
T36256 |
LC-2
LC 2,PROTAC KRASG12C Degrader-LC-2,LC2 |
PROTACs | PROTAC |
LC-2 (PROTAC KRASG12C Degrader-LC-2) 是一种新型基于von Hippel-Lindau的内源性 KRAS G12C 的 PROTAC 降解剂,DC50 在 0.25 和 0.76 μM 之间。LC-2 是一种与 MRTX849 共价结合 KRAS G12C 并招募 E3 连接酶 VH的 PROTAC,诱导 KRAS G12C 快速持续降解。LC-2 对纯合和杂合子 KRAS G12C 细胞系 MAPK 信号有抑制作用。 | |||
T8745 |
PROTAC BRAF-V600E degrader-1
Compound 23 |
Raf; PROTACs | MAPK; PROTAC |
PROTAC BRAF-V600E degrader-1 (Compound 23) 选择性地诱导 BRAF-V600E 的降解,而不是野生型 BRAF。 | |||
T39685 |
PCSK9 degrader 1
|
Others | Others |
PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function. | |||
T74982 |
Akt3 degrader 1
|
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Akt3 degrader 1 是一种特异性 Akt3 降解剂,具有抗癌抗增殖活性,可抑制小鼠体内肿瘤的生长。Akt3 degrader 1 可用于研究非小细胞肺癌和胰腺癌。 | |||
T39837 |
PROTAC ERRα Degrader-3
|
PROTACs | PROTAC |
PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein. At a concentration of 30 nM, this compound exhibits a remarkable degradation capability, reducing the ERRα protein levels by >80%. Importantly, PROTAC ERRα Degrader-3 shows no activity against the ERRβ and ERRγ proteins. | |||
T5439 |
BRD4 degrader AT1
|
Epigenetic Reader Domain; PROTACs | Chromatin/Epigenetic; PROTAC |
BRD4 degrader AT1 是基于 PROTAC 技术的高选择性 Brd4 降解剂,在细胞中对 Brd4BD2 的 Kd 为 44 nM。 | |||
T13845 |
PROTAC PARP1 degrader
|
Others | Others |
PROTAC PARP1 degrader is a degrader of PARP1 based on the PROTAC technology. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line (IC50 of 6.12 μM). | |||
T36243 |
PROTAC RIPK degrader-6
|
PROTACs | PROTAC |
PROTAC RIPK degrader-6 (example 1) is a PROTAC designed for the targeted degradation of RIP Kinase, featuring a RIP2 kinase inhibitor connected through a linker to a cereblon binder[1]. | |||
T83652 |
Cyclin K degrader 1
|
Others | Others |
Cyclin K degrader 1 是 Cyclin K 降解剂。Cyclin K degrader 1是由AT-7519转变而来的降解剂,对 Cyclin K 降解活性较弱,但不会导致降解亲和力持续下降。 | |||
T39374 |
PROTAC BET Degrader-10
|
PROTACs | PROTAC |
PROTAC BET Degrader-10 (WO2017007612A1, example 37) is a highly efficient and selective small molecule compound designed to degrade BET protein BRD4. PROTAC BET Degrader-10 functions by utilizing specific ligands that connect Cereblon and BRD4, with a DC 50 value of 49 nM. | |||
T18609 |
PROTAC ERRα Degrader-2
|
Others | Others |
PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1]. | |||
T5438 |
PROTAC CDK9 Degrader-1
|
CDK; PROTACs | Cell Cycle/Checkpoint; PROTAC |
PROTAC CDK9 Degrader-1 是一种选择性 CDK9 降解剂,是由Cereblon 配体和CDK 配体相连的PROTAC。 | |||
T12560 |
PROTAC BRD9 Degrader-1
|
Epigenetic Reader Domain; PROTACs | Chromatin/Epigenetic; PROTAC |
PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader with IC50 of 13.5 nM. | |||
T18632 |
PROTAC MDM2 Degrader-2
|
Others; PROTACs | Others; PROTAC |
PROTAC MDM2 Degrader-2 is a compound designed utilizing PROTAC technology, functioning as a MDM2 degrader. Comprised of a highly potent inhibitor targeting MDM2, a linker, and the MDM2 ligand for E3 ubiquitin ligase, this compound facilitates the degradation of MDM2[1]. | |||
T18631 |
PROTAC MDM2 Degrader-1
|
Others; PROTACs | Others; PROTAC |
PROTAC MDM2 Degrader-1 is a chemical compound that utilizes PROTAC technology to degrade MDM2. This compound is comprised of a highly effective MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1]. | |||
T18635 |
PROTAC RAR Degrader-1
|
Others; PROTACs | Others; PROTAC |
PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1]. | |||
T18605 |
PROTAC ERα Degrader-2
|
Others; PROTACs | Others; PROTAC |
PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1]. | |||
T12553 |
PROTAC EED degrader-1
|
Others; PROTACs | Others; PROTAC |
PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17. | |||
T13833 |
PROTAC BRD4 Degrader-1
|
Epigenetic Reader Domain; PROTACs | Chromatin/Epigenetic; PROTAC |
PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM). | |||
T18634 |
PROTAC MDM2 Degrader-4
|
Others | Others |
PROTAC MDM2 Degrader-4 is a compound designed using PROTAC technology to degrade MDM2. It combines a powerful MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1]. | |||
T13847 |
PROTAC SGK3 degrader-1
SGK3-PROTAC1 |
SGK; PROTACs | Metabolism; PROTAC |
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 是一种靶向 SGK3 且与 VH032 VHL 结合配体的 PROTAC 偶联物,可诱导内源性 SGK3 降解。PROTAC SGK3 degrader-1 可抑制GDC0941诱导的癌细胞增殖。 | |||
T13840 |
PROTAC FAK degrader 1
|
Others; PROTACs | Others; PROTAC |
PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM). | |||
T13835 |
PROTAC BRD4 Degrader-3
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4. | |||
T13834 | PROTAC BRD4 Degrader-2 | Epigenetic Reader Domain | Chromatin/Epigenetic |
PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM). | |||
T16667 |
PROTAC Sirt2 Degrader-1
|
Sirtuin; PROTACs | Chromatin/Epigenetic; DNA Damage/DNA Repair; PROTAC |
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 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]. | |||
T11975 |
PROTAC Mcl1 degrader-1
|
BCL; PROTACs | Apoptosis; PROTAC |
PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM. | |||
T17728 |
PROTAC CDK9 degrader-2
|
Others | Others |
PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. | |||
T10485 |
PROTAC Bcl2 degrader-1
|
BCL; PROTACs | Apoptosis; PROTAC |
PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM). |