Bis-PEG5-acid (PROTAC Linker 36) is a PROTAC linker, which belongs to a polyethylene glycol (PEG) linker. Bis-PEG5-acid (PROTAC Linker 36) can be used in the synthesis of the CP5V. CP5V is a PROTAC, and specifically degrades Cdc20[1].
IC50 & Target
PEGs
分子量
338.35
Formula
C14H26O9
CAS 号
439114-13-3
运输条件
Room temperature in continental US; may vary elsewhere.
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 (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC[1].
IC50 & Target[1]
CDK9
17 μM (IC50, MCF-7 cells)
分子量
748.74
Formula
C39H36N6O10
CAS 号
2435721-30-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.
PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136)[1].
IC50 & Target
BRD4
体外研究 (In Vitro)
PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC50 of 14.2 nM against BRD4 BD1[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
371.43
Formula
C23H21N3O2
CAS 号
2101200-10-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228.
PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader[1].
IC50 & Target
VHL
Cereblon
分子量
1061.25
Formula
C53H72N8O13S
CAS 号
2358775-70-7
运输条件
Room temperature in continental US; may vary elsewhere.
3-Maleimidopropionic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
Alkyl-Chain
体外研究 (In Vitro)
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].
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.
分子量
169.13
Formula
C7H7NO4
CAS 号
7423-55-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
Cystamine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
Alkyl-Chain
体外研究 (In Vitro)
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].
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.
分子量
152.28
Formula
C4H12N2S2
CAS 号
51-85-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4 (IRAK4). PROTAC IRAK4 ligand-1 can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966)[1].
分子量
612.56
Formula
C29H27F3N6O6
CAS 号
2357108-39-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 12.5 mg/mL (20.41 mM; ultrasonic and warming and heat to 60°C)
PROTAC ERα Degrader-2 comprises a IAP 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].
IC50 & Target
ERα
cIAP1
分子量
763.96
Formula
C42H61N5O8
CAS 号
1351169-29-3
运输条件
Room temperature in continental US; may vary elsewhere.
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader[1].
IC50 & Target[1]
VHL
FKBP
体外研究 (In Vitro)
PROTAC treatment time courses demonstrated a notable increase in polyubiquitination of EGFP-FKBP in response to treatment with 250 nM of PROTAC FKBP Degrader-3 (compound 10) for VHL within the first hour. Upon recruiting endogenous VHL via PROTAC FKBP Degrader-3 (compound 10), only one EGFP background lysine (Lys158) is found to be ubiquitylated[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.
分子量
1295.54
Formula
C68H90N6O17S
CAS 号
2079056-43-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Ottis P, et al. Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation. ACS Chem Biol. 2017 Oct 20;12(10):2570-2578.
PROTAC BRD4 degrader for PAC-1 (compound 5),是一种用于 PAC 的 PROTAC- linker 偶联物,包含嵌合体 BET 降解剂 GNE-987 和含二硫化物的 linker。
PROTAC BRD4 degrader for PAC-1 Chemical Structure
规格
价格
是否有货
数量
1 mg
¥18000
In-stock
5 mg
询价
10 mg
询价
* Please select Quantity before adding items.
生物活性
PROTAC BRD4 degrader for PAC-1 (compound 5), a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 and disulfide-containing linker[1].
分子量
1306.58
Formula
C62H77F2N9O12S4
运输条件
Room temperature in continental US; may vary elsewhere.
PEG3-O-CH2COOH (PROTAC Linker 8) is a PEG-based PROTAC linker can be used in the synthesis of SNIPERs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
PEG3-O-CH2COOH (Compound 15b) is a PROTAC linker can be used in the synthesis of a series of SNIPER(ER)s. SNIPERs that recruit inhibitor of the apoptosis protein (IAP) ubiquitin ligases to specifically degrade targeted proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
208.21
Formula
C8H16O6
CAS 号
51951-05-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[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.
Tetraethylene glycol (PROTAC Linker 18) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
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.
分子量
194.23
Formula
C8H18O5
CAS 号
112-60-7
中文名称
三缩四乙二醇
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.
369-Trioxaundecanedioic Acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
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].
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.
分子量
222.19
Formula
C8H14O7
CAS 号
13887-98-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 12.5 mg/mL (56.26 mM; ultrasonic and warming and heat to 60°C)
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
Triethylene glycol (PROTAC Linker 25) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
IC50 & Target[1]
PEGs
体外研究 (In Vitro)
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.
分子量
150.17
Formula
C6H14O4
CAS 号
112-27-6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.
PROTAC BET Degrader-1 是由Cereblon配体和BET配体相连的PROTAC,能够在低浓度下降低 BRD2,BRD3 和 BRD4 的蛋白水平。
PROTAC BET Degrader-1 Chemical Structure
CAS No. : 2093386-22-0
规格
价格
是否有货
数量
5 mg
¥5500
In-stock
10 mg
¥8500
In-stock
25 mg
¥18500
In-stock
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
PROTAC BET Degrader-1 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
生物活性
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
IC50 & Target
BET[1]
体外研究 (In Vitro)
PROTAC BET Degrader-1 (Compound 9) is a potent BET degrader based on PROTAC, decreases the level of BRD2, BRD3, and BRD4 proteins in RS4;11 cells at 3-10 nM, and inhibits the growth of this cell line with an IC50 of 4.3 nM, and 45.5 nM for MOLM-13 cells[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.
分子量
871.90
Formula
C44H45N11O9
CAS 号
2093386-22-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
NH2-Ph-C4-acid-NH2-Me (PROTAC Linker 31) is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTACs[1].
IC50 & Target
Alkyl-Chain
体外研究 (In Vitro)
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.
分子量
222.28
Formula
C12H18N2O2
CAS 号
1263819-48-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Leverett CA, et al. Design, Synthesis, and Cytotoxic Evaluation of Novel Tubulysin Analogues as ADC Payloads. ACS Med Chem Lett. 2016 Aug 26;7(11):999-1004.
PROTAC BET Degrader-10 是有效 BET BRD4降解剂,由Cereblon配体和BRD4配体相连,DC50 为 49 nM,详细信息请参考专利 WO2017007612A1,example 37。
PROTAC BET Degrader-10 Chemical Structure
CAS No. : 1957234-97-7
规格
价格
是否有货
数量
10 mM * 1 mL in DMSO
¥4140
In-stock
5 mg
¥3000
In-stock
10 mg
¥4800
In-stock
25 mg
¥9000
In-stock
50 mg
¥13500
In-stock
100 mg
¥20000
In-stock
200 mg
询价
500 mg
询价
* Please select Quantity before adding items.
PROTAC BET Degrader-10 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
生物活性
PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, connected by ligands for Cereblon and BRD4, with a DC50 of 49 nM[1].
分子量
783.29
Formula
C39H39ClN8O6S
CAS 号
1957234-97-7
运输条件
Room temperature in continental US; may vary elsewhere.
PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
IC50 & Target[1]
cIAP1
体外研究 (In Vitro)
Specific and Nongenetic IAPs-dependent Protein Erasers (SNIPERs) are bifunctional compounds which are designed by conjugating an IAPs-recognition structure with a target protein-recognition structure. Targeting proteins for degradation involves three steps. 1, its two recognition structures allow SNIPER to form a complex linking IAPs, which have E3 ligase activity, with the target protein. 2, the target protein is polyubiquitinated by IAPs. 3, the polyubiquitinated protein is degraded by proteasome.
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.
分子量
884.03
Formula
C45H68F3N3O11
运输条件
Room temperature in continental US; may vary elsewhere.