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PROTAC
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Ligands for Target Protein for PROTAC
PROTACs consist of two covalently linked protein-binding molecules: one capable of engaging an E3 ubiquitin ligase, and another that binds to a target protein meant for degradation. The ligand for target protein will lead to attachment of a PROTAC to the proteins of interest for ubiquitin and subsequent degradation.
- (+)-JQ-1T21101268524-70-4(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1 2) (IC50=77 33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
- $30
SizeQTY
Cited - QuizartinibT2066950769-58-1Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.
- $53
SizeQTY Cited - IbrutinibT1835936563-96-1Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
- $36
SizeQTY Cited - AR antagonist 1T103591818885-54-9AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.
- $133
SizeQTY
- CPI-0610 carboxylic acidT108791380089-81-5In houseCPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.
- $526
SizeQTY - PROTAC BRD4 ligand-1T125512313230-51-0In housePROTAC BRD4 ligand-1 is a ligand for PROTAC GNE-987 targeting the BRD4 protein and is an inhibitor of BET.
- $125
SizeQTY - TMX-4153T809742867519-91-1TMX-4153 is a bivalent degrader that selectively targets and rapidly degrades endogenous PIP4K2C through recruitment of the von Hippel-Lindau (VHL) E3 ligase complex, demonstrating a K D of 42 nM. It is applicable in the synthesis of PROTAC [1].
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SizeQTY - Abemaciclib metabolite M18T739092704316-81-2Abemaciclib metabolite M18 (LSN3106729) is a potent cyclin-dependent kinase (CDK) inhibitor with antitumor properties. It has been incorporated alongside a cereblon (CRBN) ligand to develop a proteolysis-targeting chimera (PROTAC) that selectively degrades CDK4/6 [1] [2].
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SizeQTY - SMD-3040 TFAT81147SMD-3040 TFA is a selective SMARCA2 degrader comprising SMARCA2/4 ligands, a linker, and VHL ligands, utilized in PROTAC drug synthesis. It demonstrates robust tumor growth inhibition in tumor xenograft models [1].
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SizeQTY - CFT1946T779722882165-79-7CFT1946 is a selective and orally active ligand targeting BRAF kinase, functioning as a degrader of mutant BRAF forms including BRAFV600E, G469A, G466V, and p61-BRAFV600E. It is utilized in tumor research [1].
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SizeQTY - PROTAC PTK6 ligand-1T779282408341-98-8PROTAC PTK6 ligand-1 serves as an intermediate in the synthesis of BTK kinase inhibitors [1] and is utilized in the preparation of ARD-61 [2].
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SizeQTY - AZD9496 deacrylic acid phenolT779852173404-70-9AZD9496 deacrylic acid phenol (AZD9496) represents a portion of the ligand that targets the protein for PROTAC ER Degrader-4 [1].
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SizeQTY - BI-4464T54801227948-02-8BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC
- $52
SizeQTY - UNC6852T139542688842-08-0UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.
- $135
SizeQTY - PROTAC BRD4 ligand-2 hydrochlorideT77921PROTAC BRD4 Ligand-2 Hydrochloride serves as a ligand targeting the BRD4 protein, specifically designed for use with PROTAC CFT-2718.
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SizeQTY - DUPAT19301302941-52-2DUPA (N,N''-Carbonylbis[L-glutamic acid]) is used as the targeting moiety to actively deliver DTX for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.
- $37
SizeQTY - Dasatinib carbaldehydeT185952112837-79-1Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) is based on Dasatinib which is an ABL inhibitor, binds to the IAP ligand via a linker, and forms SNIPER [1].
- $48
SizeQTY - Tazemetostat de(methyl morpholine)-COOHT779402685873-44-1Tazemetostat de(methyl morpholine)-COOH (compound 7), a PROTAC ligand for EZH2, facilitates the synthesis of PROTACs that target this enzyme. These EZH2 degraders exhibit potent inhibition of cell viability in diffuse large B-cell lymphoma (DLBCL) and other lymphoma subtypes [1].
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SizeQTY - Navitoclax-piperazineT121862143096-93-7Navitoclax-piperazine (ABT-263-piperazine) is an inhibitor of B-cell lymphoma extra large (BCL-XL).
- $158
SizeQTY
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