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| Product | Description | |
|---|---|---|
| A01 | A01 is a high affinity Smurf1 E3 ubiquitin ligase inhibitor (Kd = 3.7 nM), which attenuates Smurf1-mediated Smad 1/5 degradation and enhances BMP signaling. Study showed that it potentiated BMP-2-induced osteoblastic activity in C2C12 myoblasts and MC3T3-E1 osteoblast precursor cells. Group: Pharmaceutical. Alternative Names: Smurf1-IN-A01; Smurf1INA01; Smurf1 IN A01; Smurf1 inhibitor A01; Smurf1-inhibitor-A01; A01; A 01; A-01; [4-[[4-Chloro-3-(trifluoromethyl)phenyl]sulfonyl]-1-piperazinyl][4-(5-methyl-1H-pyrazol-1-yl)phenyl]methanone; SMURF1 inhibitor A01. CAS No. 1007647-73-5. Pack Sizes: 1mg;1g;10g. Product ID: 1007647-73-5. Molecular formula: C22H20ClF3N4O3S. Mole weight: 512.93. Custom synthesis is available. Send your inquiries for more information. |  London |
| ACBI1 | ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis. Group: Pharmaceutical. Alternative Names: ACBI 1; ACBI-1; (2S,4R)-N-(2-(2-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenoxy)ethoxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide. CAS No. 2375564-55-7. Pack Sizes: 1mg;1g;10g. Product ID: 2375564-55-7. Molecular formula: C49H58FN9O7S. Mole weight: 936.12. Custom synthesis is available. Send your inquiries for more information. | London |
| ARV-825 | ARV-825 is a BRD4 inhibitor based on PROTAC technology. ARV-825 recruits BRD4 to E3 ubiquitin ligase cereblon, resulting in the degradation of BRD4. In post-myeloproliferative neoplasm secondary (s) AML cell lines, treatment with ARV-825 induces apoptosis and inhibits cell proliferation. Group: Pharmaceutical. Alternative Names: 2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethoxy)phenyl)acetamide. CAS No. 1818885-28-7. Pack Sizes: 100 mg. Product ID: B1370-474664. Molecular formula: C46H47ClN8O9S. Mole weight: 923.44. Custom synthesis is available. Send your inquiries for more information. | London |
| AT-406 | AT-406 is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3 (with Ki of 66.4 nM), cIAP1-BIR3(with Ki of 1.9 nM) and cIAP2-BIR3 (with Ki of 5.1 nM), respectively. Group: Pharmaceutical. Alternative Names: AT406; AT 406; SM-406; SM 406; SM406; ARRY-334543; ARRY 334543; ARRY334543. CAS No. 1071992-99-8. Pack Sizes: 100 mg. Product ID: B0084-454116. Molecular formula: C32H43N5O4. Mole weight: 561.71. Custom synthesis is available. Send your inquiries for more information. | London |
| CC-885 | CC-885 is a cereblon (CRBN) modulator with an anti-tumour activity mediated through the cereblon-dependent ubiquitination and degradation of the translation termination factor GSPT1. CC-885 potently suppresses the proliferation of human acute myeloid leukaemia (AML) tumour cell lines. Uses: Antitumor agent. Group: Pharmaceutical. Alternative Names: CC 885; CC885; N-(3-chloro-4-methylphenyl)-N'-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-5-yl]methyl]-urea. CAS No. 1010100-07-8. Pack Sizes: 100 mg. Product ID: B2693-054699. Molecular formula: C22H21ClN4O4. Mole weight: 440.88. Custom synthesis is available. Send your inquiries for more information. | London |
| dBET1 | dBET1 is a potent BRD4 protein degrader composed of a BET bromodomain inhibitor (+)-JQ1 and a sedative drug thalidomide. The (+)-JQ1 portion binds to the BET bromodomains, and the thalidomide binds to cereblon to form a cereblon E3 ubiquitin ligase complex, inducing cereblon-dependent BET protein degradation. Group: Pharmaceutical. Alternative Names: (6S)-4-(4-chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide. CAS No. 1799711-21-9. Pack Sizes: 50 mg. Product ID: B1370-285214. Molecular formula: C38H37ClN8O7S. Mole weight: 785.27. Custom synthesis is available. Send your inquiries for more information. | London |
| Lenalidomide | Cereblon binder; induces ubiquitination and degradation of CK1a and transcription factors IKZF1, IKZF3 and SALL4 by E3 ubiquitin ligase. Group: Pharmaceutical. Alternative Names: CC5013; CC-5013; CC 5013; IMiD1; Lenalidomide; US brand name: Revlimid. CAS No. 191732-72-6. Pack Sizes: 25 g. Product ID: NP3322. Molecular formula: C13H13N3O3. Mole weight: 259.26. Custom synthesis is available. Send your inquiries for more information. | London |
| Mezigdomide | Mezigdomide is a new type of protein degrading agent, a cereblon E3 ubiquitin ligase modulating drug, with potential immunomodulatory and anti-tumor activity. Group: Pharmaceutical. Alternative Names: CC-92480; CC 92480; CC92480; (S)-4-(4-(4-(((2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile. CAS No. 2259648-80-9. Pack Sizes: 100 mg. Product ID: B1370-372913. Molecular formula: C32H30FN5O4. Mole weight: 567.6. Custom synthesis is available. Send your inquiries for more information. | London |
| P22077 | P22077 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor. P22077 potently induces apoptosis in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression. P22077 was found to be able to sensitize chemoresistant LA-N-6 NB cells to chemotherapy. In an in vivo orthotopic NB mouse model, P22077 significantly inhibited the xenograft growth of three NB cell lines. USP7-specific inhibitors like P22077 may serve not only as a stand-alone therapy but also as an effective adjunct to current chemotherapeutic regimens for treating NB with an intact USP7-HDM2-p53 axis. Group: Pharmaceutical. Alternative Names: P-22077; P 22077. CAS No. 1247819-59-5. Pack Sizes: 100 mg. Product ID: B0084-462597. Molecular formula: C12H7F2NO3S2. Mole weight: 315.309. Custom synthesis is available. Send your inquiries for more information. | London |
| Pomalidomide-C2-NH2 | Pomalidomide-C2-NH2 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 17 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1]. Group: Pharmaceutical. Alternative Names: 4-((2-aminoethyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione; SCHEMBL17884390; TQP0427; Cereblon Ligand-Linker Conjugates 15; HY-128846; Pomalidomide-C2-NH2; Pomalidomide-alkylC2-amine; E3 ligase Ligand 17; 4-[(2-Aminoethyl)amino]-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione hydrochloride. CAS No. 1957235-66-3. Pack Sizes: 25 mg. Product ID: BAT-006493. Molecular formula: C15H16N4O4. Mole weight: 316.31. Custom synthesis is available. Send your inquiries for more information. | London |
| Pseudolaric acid B | Pseudolaric acid B (PAB), which comes from the bark of Pseudolarix kaempferi Gordon, has diverse effects that are relevant to cancer therapy, including apoptosis of cancer cells (IC50 = ~1 μM), preventing angiogenesis, and inhibiting tumor growth in vivo. pseudolaric acid B can trigger apoptosis by decreasing Bcl-2 levels and activating caspase-3 protease. The future development of PAB as a cancer therapeutic is ongoing. Besides, PAB significantly suppressed proliferation of DU145 cells in a dose-dependent manner without obvious cytotoxicity. PAB may inhibit growth of HRPC DU145 cells and induce apoptosis through ROS generation and Bcl-2 degradation via the activation of the ubiquitin-proteasome pathway. Uses: Antifungal/antifertility. Group: Pharmaceutical. Alternative Names: PLAB; 1H-4,9a-Ethanocyclohepta[c]pyran-7-carboxylicacid,4a-(acetyloxy)-3-[(1E,3E)-4-carboxy-1,3-pentadien-1-yl]-3,4,4a,5,6,9-hexahydro-3-methyl-1-oxo-,7-methyl ester, (3R,4S,4aS,9aR)-; Pseudolarix acid B; Pseudolaric acid. CAS No. 82508-31-4. Pack Sizes: 10 mg. Product ID: NP1536. Molecular formula: C23H28O8. Mole weight: 432.46. Custom synthesis is available. Send your inquiries for more information. | London |
| RAMB4 | RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. Group: Pharmaceutical. Alternative Names: PTP1B-IN-9; 3,5-bis(3,4-dichlorobenzylidene)piperidin-4-one. CAS No. 145888-79-5. Pack Sizes: 25 mg. Product ID: B1370-063301. Molecular formula: C19H13Cl4NO. Mole weight: 413.13. Custom synthesis is available. Send your inquiries for more information. | London |
| (S,R,S)-AHPC-Me | E3 ligase Ligand 1A is a VH032 derivate for conjugation reactions of PROTAC, which can hijack VHL as the E3 ubiquitin ligase component. Group: Pharmaceutical. Alternative Names: (S,R,S)-AHPC-Me; VHL ligand 2; E3 ligase Ligand 1A; 1-(2-amino-3,3-dimethylbutanoyl)-4-hydroxy-N-[1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide. CAS No. 1948273-02-6. Pack Sizes: 1 g. Product ID: B2693-291831. Molecular formula: C23H32N4O3S. Mole weight: 444.59. Custom synthesis is available. Send your inquiries for more information. | London |
| TAK-243 | TAK-243, a pyrazolopyrimidine derivative, has been found to be an Ubiquitin-protein ligase inhibitor and was just finished the Phase-I trial against solid tumors. Group: Pharmaceutical. Alternative Names: TAK-243; TAK 243; TAK243; MLN7243; MLN-7243; MLN 7243; AOB87172; AOB-87172; AOB 87172. CAS No. 1450833-55-2. Pack Sizes: 25 mg. Product ID: B2693-475793. Molecular formula: C19H20F3N5O5S2. Mole weight: 519.51. Custom synthesis is available. Send your inquiries for more information. | London |
| TCID | TCID is a DUB inhibitor for ubiquitin C-terminal hydrolase L3 with IC50 of 0.6 μM, 125-fold selective to L1. Group: Pharmaceutical. Alternative Names: 4,5,6,7-Tetrachloroindan-1,3-dione; UCH-L3 Inhibitor. CAS No. 30675-13-9. Pack Sizes: 100 mg. Product ID: B2693-089799. Molecular formula: C9H2Cl4O2. Mole weight: 283.92. Custom synthesis is available. Send your inquiries for more information. | London |
| Thalidomide, propargyl | Thalidomide, propargyl is a cereblon-recruiting ligand consisting of an E3 ubiquitin ligase thalidomide conjugated to an alkyne linker ready for a target protein ligand. It has been used in PROTAC technology for target protein degradation. Group: Pharmaceutical. Alternative Names: 2-(2,6-Dioxo-3-piperidinyl)-4-(2-propyn-1-yloxy)-1H-isoindole-1,3(2H)-dione. CAS No. 2098487-39-7. Pack Sizes: 1 g. Product ID: B2693-285284. Molecular formula: C16H12N2O5. Mole weight: 312.28. Custom synthesis is available. Send your inquiries for more information. | London |
| VH-298 | VH-298 is a high-affinity inhibitor of E3 ubiquitin ligase VHL (Kd value of 80-90 nM) that could block VHL and HIF-α interactions. VH-298 can be used in PROTAC technology. Uses: Enzyme inhibitors. Group: Pharmaceutical. Alternative Names: (2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide; EX-A1505; VH 298; VH298; VH-298. CAS No. 2097381-85-4. Pack Sizes: 50 mg. Product ID: B2693-170543. Molecular formula: C27H33N5O4S. Mole weight: 523.65. Custom synthesis is available. Send your inquiries for more information. | London |
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