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| Product | Description | |
|---|---|---|
| AAL-993 | AAL-993 is a VEGFR tyrosine kinase inhibitor that possesses dual inhibition of VEGFR signaling and HIF-1α expression through ERK inhibition without affecting Akt phosphorylation. Group: Pharmaceutical. Alternative Names: AAL 993; AAL993; 2-((4-pyridyl)methyl)amino-N-(3-(trifluoromethyl)phenyl)benzamide. CAS No. 269390-77-4. Pack Sizes: 1mg;1g;10g. Product ID: 269390-77-4. Molecular formula: C20H16F3N3O. Mole weight: 371.36. Custom synthesis is available. Send your inquiries for more information. |  London |
| AG 126 | Tyrphostins are protein tyrosine kinase inhibitors developed to inhibit cell growth through blocking the activity of certain GFRK (growth factor receptor kinases). AG 126 selectively inhibits the phosphorylation of ERK1 and ERK2 at 25-50 μM. It also inhibits the production of TNF-α (tumor necrosis factor-α), attenuating signaling through NF-κB, the induced expression of COX-2 and iNOS, and the inflammatory response in animal models. AG 126 is a poor inhibitor of epidermal GFRK with IC50 of 450 μM and platelet-derived GFRK with IC50 > 100 μM. AG 126 may represent a new approach for the therapy of inflammation. Uses: Anti- inflammation. Group: Pharmaceutical. Alternative Names: AG126; AG-126; Tyrphostin AG 126; UNII-7YA4AMD1JC; Tyrphostin A 10; alpha-Cyano-(3-hydroxy-4-nitro)cinnamonitrile. CAS No. 118409-62-4. Pack Sizes: 100 mg. Product ID: B1370-195904. Molecular formula: C10H5N3O3. Mole weight: 215.16. Custom synthesis is available. Send your inquiries for more information. | London |
| α-Amyrin | α-Amyrin is a triterpenoid that has been found in B. copallifera and has diverse biological activities. It activates the ERK and GSK-3β signaling pathways. α-Amyrin is a potential protein kinase A inhibitor. Group: Pharmaceutical. Alternative Names: Viminalol; alpha-Amyrenol; Urs-12-en-3beta-ol; (3β)-urs-12-en-3-ol. CAS No. 638-95-9. Pack Sizes: 10 mg. Product ID: B1370-147265. Molecular formula: C30H50O. Mole weight: 426.73. Custom synthesis is available. Send your inquiries for more information. | London |
| AZD0364 | AZD-0364 is a potent and selective ERK2 inhibitor, which has an IC50 value of 0.6 nM. AZD-0364 is measured in the A375 phospho-p90RSK assays with IC50s of 5.7 nM. AZD-0364 can inhibit the growth of a panel of cancer cell lines. The combination of Selumetinib and AZD-0364 ethanesulfonic acid results in a reduction in tumor growth. Group: Pharmaceutical. Alternative Names: AZD-0364; AZD 0364; tizaterkib. CAS No. 2097416-76-5. Pack Sizes: 25 mg. Product ID: B2693-291616. Molecular formula: C24H24F2N8O2. Mole weight: 494.5. Custom synthesis is available. Send your inquiries for more information. | London |
| Chrysophanol | Chrysophanic acid (Chrysophanol) is a natural anthraquinone with anticancer activity in EGFR-overexpressing SNU-C5 human colon cancer cells. Chrysophanic acid preferentially blocked proliferation in SNU-C5 cells but not in other cell lines (HT7, HT29, KM12C, SW480, HCT116 and SNU-C4) with low levels of EGFR expression. Chrysophanic acid treatment in SNU-C5 cells inhibited EGF-induced phosphorylation of EGFR and suppressed activation of downstream signaling molecules, such as AKT, extracellular signal-regulated kinase (ERK) and the mammalian target of rapamycin (mTOR)/ribosomal protein S6 kinase (p70S6K). Chrysophanic acid (80 and 120 μm) significantly blocked cell proliferation when combined with the mTOR inhibitor, rapamycin. These findings offer the first evidence of anticancer activity for chrysophanic acid via EGFR/mTOR mediated signaling transduction pathway. Chrysophanol is a natural compound found in the roots and rhizomes of Rheum palmatum L. It can be used in cosmetics material. Uses: Anti-inflammatory. Group: Pharmaceutical. Alternative Names: 1,8-dihydroxy-3-methylanthracene-9,10-dione. CAS No. 481-74-3. Pack Sizes: 1 g. Product ID: NP0901. Molecular formula: C15H10O4. Mole weight: 254.24. Custom synthesis is available. Send your inquiries for more information. | London |
| Corynoxeine | Corynoxeine is a potent ERK1/2 inhibitor of key PDGF-BB-induced VSMC proliferation and a useful and prospective compound in the prevention and treatment for vascular diseases. Uses: Antihypertension. Group: Pharmaceutical. Alternative Names: corynoxeine; (7R,16E,20α)-16,17,18,19-Tetradehydro-17-methoxy-2-oxocorynoxan-16-carboxylic acid methyl ester; (alphaE,1'R,6'R,7'S,8'aS)-6'-Ethenyl-1,2,2',3',6',7',8',8'a-octahydro-alpha-(methoxymethylene)-2-oxospiro[3H-indole-3,1'(5'H)-indolizine]-7'-acetic acid methyl ester; 16,17,18,19-Tetradehydro-17-methoxy-2-oxocorynoxan-16-carboxylic acid methyl ester; Spiro[3H-indole-3,1'(5'H)-indolizine]-7'-aceticacid, 6'-ethenyl-1,2,2',3',6',7',8',8'a-octahydro-a-(methoxymethylene)-2-oxo-, methyl ester, (aE,1'R,6'R,7'S,8'aS)-. CAS No. 630-94-4. Pack Sizes: 10 mg. Product ID: B2703-450788. Molecular formula: C22H26N2O4. Mole weight: 382.45. Custom synthesis is available. Send your inquiries for more information. | London |
| Defactinib | Defactinib, also known as VS-6063 and PF-04554878, is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival. The tyrosine kinase FAK is , a signal transducer for integrins that is upregulated in many tumor cell types and is involved in tumor cell invasion, migration and proliferation. Group: Pharmaceutical. Alternative Names: N-methyl-4-((4-(((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide; VS6063; VS 6063; VS-6063; PF04554878; PF-04554878; PF 04554878; PF4554878; PF-4554878. CAS No. 1073154-85-4. Pack Sizes: 200 mg. Product ID: B0084-462762. Molecular formula: C20H21F3N8O3S. Mole weight: 510.496. Custom synthesis is available. Send your inquiries for more information. | London |
| DEL-22379 | DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ?0.5 μM. Group: Pharmaceutical. Alternative Names: DEL-22379; DEL 22379; DEL22379. CAS No. 181223-80-3. Pack Sizes: 25 mg. Product ID: B0084-470902. Molecular formula: C26H28N4O3. Mole weight: 444.53. Custom synthesis is available. Send your inquiries for more information. | London |
| Encorafenib | Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of LGX818 may result in a decrease in proliferation of tumor cells. The Raf mutation BRAF V600E is frequently upregulated in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival. Group: Pharmaceutical. Alternative Names: LGX818; LGX-818; LGX 818; Methyl N-[(2S)-1-[[4-[3-[5-chloro-2-fluoro-3-(methanesulfonamido)phenyl]-1-propan-2-ylpyrazol-4-yl]pyrimidin-2-yl]amino]propan-2-yl]carbamate. CAS No. 1269440-17-6. Pack Sizes: 150 mg. Product ID: B0084-462563. Molecular formula: C22H27ClFN7O4S. Mole weight: 540.011. Custom synthesis is available. Send your inquiries for more information. | London |
| FIPI | FIPI, a derivative of halopemide, is a potent and selective phospholipase D (PLD) inhibitor with IC50 values of 20 and 25 nM for PLD2 and PLD1 respectively. It attenuate mercury-induced lipid signaling leading to protection against cytotoxicity in aortic endothelial cells. It rapidly blocks in vivo PA production with subnanomolar potency. It has good pharmacokinetic parameters in rats. It did not significantly inhibit p38 or ERK phosphorylation in bone marrow-derived macrophages stimulated with lipopolysaccharide. It prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. Group: Pharmaceutical. Alternative Names: 5-Fluoro-2-Indolyl des-Chlorohalopemide; N-[2-[4-(2,3-Dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-5-fluoro-1H-indole-2-carboxamide; 5-Fluoro-N-(2-(4-(2-Oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-1H-indole-2-carboxamide. CAS No. 939055-18-2. Pack Sizes: 100 mg. Product ID: B2693-438324. Molecular formula: C23H24FN5O2. Mole weight: 421.47. Custom synthesis is available. Send your inquiries for more information. | London |
| GDC-0994 | GDC-0994, also known as RG7842, is an orally available inhibitor of extracellular signal-regulated kinase (ERK), with potential antineoplastic activity. Upon oral administration, GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. This prevents ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival. Uses: Antineoplastic agents. Group: Pharmaceutical. Alternative Names: GDC0994; GDC 0994; RG7842; RG-7842; RG 7842; Ravoxertinib. CAS No. 1453848-26-4. Pack Sizes: 50 mg. Product ID: B2693-462528. Molecular formula: C21H18ClFN6O2. Mole weight: 440.863. Custom synthesis is available. Send your inquiries for more information. | London |
| Haginin A | Haginin A is a natural compound isolated from the aerial parts of Lespedeza cyrtobotrya. Haginin A has radical scavenging activity and mushroom tyrosinase inhibitory activity. Haginin A is an effective inhibitor of hyperpigmentation caused by UV irradiation or by pigmented skin disorders through downregulation via ERK and Akt/PKB activation, MITF, and also by the subsequent downregulation of tyrosinase and TRP-1 production. Group: Pharmaceutical. Alternative Names: 7,4'-Dihydroxy-2',3'-dimethoxyisoflavene. CAS No. 74174-29-1. Pack Sizes: 5 mg. Product ID: NP2192. Molecular formula: C17H16O5. Mole weight: 300.31. Custom synthesis is available. Send your inquiries for more information. | London |
| Lyoniresinol | Lyoniresinol, a natural lignan isolated from the root of Vitex negundo,is one of the eight lignans purified from methanol which has robust tyrosinase inhibitory capacity. Lyoniresinol exhibits the activity of antioxidative, and it decreases tyrosinase activity and melanin biosynthesis in B16F10 cells by activating ERK signaling, which downregulates MITF, tyrosinase, but not TRP-1 and TRP-2 protein expression, it can perhaps be incorporated into clinical dermatologic use as a skin lightening agent. Uses: Anti-melanogenic; anti-oxidant. Group: Pharmaceutical. Alternative Names: (1S)-1α-(3,5-Dimethoxy-4-hydroxyphenyl)-6,8-dimethoxy-7-hydroxy-1,2,3,4-tetrahydronaphthalene-2β,3α-dimethanol. CAS No. 14464-90-5. Pack Sizes: 1 mg. Product ID: NP3922. Molecular formula: C22H28O8. Mole weight: 420.5. Custom synthesis is available. Send your inquiries for more information. | London |
| MG-132 | MG-132 is a potent Proteasome inhibitor with potential anticancer activity. MG-132 induces MCPIP1 expression; induces C6 glioma cell apoptosis via oxidative stress; induces AIF nuclear translocation through down-regulation of ERK and Akt/mTOR pathway. Group: Pharmaceutical. Alternative Names: Z-Leu-leu-leu-al. CAS No. 133407-82-6. Pack Sizes: 100 mg. Product ID: B2693-361205. Molecular formula: C26H41N3O5. Mole weight: 475.62. Custom synthesis is available. Send your inquiries for more information. | London |
| MK-8353 | MK-8353 is an orally available ERK1/2 inhibitor. It exhibited antitumor activity in patients with BRAFV600-mutant melanoma. Group: Pharmaceutical. Alternative Names: (3S)-3-(methylthio)-1-[2-[4-[4-(1-methyl-1,2,4-triazol-3-yl)phenyl]-3,6-dihydro-2H-pyridin-1-yl]-2-oxoethyl]-N-[3-(6-propan-2-yloxy-3-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide. CAS No. 1184173-73-6. Pack Sizes: 50 mg. Product ID: B2693-291615. Molecular formula: C37H41N9O3S. Mole weight: 691.84. Custom synthesis is available. Send your inquiries for more information. | London |
| Rineterkib | Rineterkib is a RAF and ERK1/2 inhibitor developed for the treatment of proliferative diseases characterized by activating mutations in the MAPK pathway. Group: Pharmaceutical. Alternative Names: ERK-IN-1; LTT-462. CAS No. 1715025-32-3. Pack Sizes: 25 mg. Product ID: B2693-373160. Molecular formula: C26H27BrF3N5O2. Mole weight: 578.4. Custom synthesis is available. Send your inquiries for more information. | London |
| SCH772984 | SCH772984 is a potent and selective ERK inhibitor with potential anticancer activity. SCH722984 showed activity against BRAF mutant, NRAS mutant and wild-type melanoma. Combining vemurafenib and SCH722984 in BRAF mutant melanoma was synergistic in a majority of cell lines and significantly delayed the onset of acquired resistance in long term in vitro assays. Therefore, SCH772984 may be clinically applicable as a treatment for non-BRAF mutant melanoma or in BRAF-mutant melanoma with innate or acquired resistance, alone or in combination with BRAF inhibitors. Group: Pharmaceutical. Alternative Names: SCH-772984; SCH 772984; (R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide. CAS No. 942183-80-4. Pack Sizes: 25 mg. Product ID: B2693-429803. Molecular formula: C33H33N9O2. Mole weight: 587.688. Custom synthesis is available. Send your inquiries for more information. | London |
| SHP099 | SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 value 0.071 μM) that stabilizes SHP2 in an auto-inhibited conformation. SHP099 suppresses signaling through the Ras-ERK pathway and blocks the proliferation of receptor tyrosine kinase-driven human cancer cells in vitro and in vivo. Group: Pharmaceutical. Alternative Names: 6-(4-amino-4-methylpiperidin-1-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine; SHP099; SHP-099; SHP 099. CAS No. 1801747-42-1. Pack Sizes: 20 mg. Product ID: B0084-007855. Molecular formula: C16H19Cl2N5. Mole weight: 352.26. Custom synthesis is available. Send your inquiries for more information. | London |
| SHP099 HCl | SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 value 0.071 μM) that stabilizes SHP2 in an auto-inhibited conformation. SHP099 suppresses signaling through the Ras-ERK pathway and blocks the proliferation of receptor tyrosine kinase-driven human cancer cells in vitro and in vivo. Group: Pharmaceutical. Alternative Names: 6-(4-amino-4-methylpiperidin-1-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine hydrochloride; SHP099; SHP-099; SHP 099. SHP-099 hydrochloride, SHP-099 HCl. CAS No. 1801747-11-4. Pack Sizes: 500 mg. Product ID: B2693-007852. Molecular formula: C16H20Cl3N5. Mole weight: 388.72. Custom synthesis is available. Send your inquiries for more information. | London |
| SIS3 HCl | SIS3 is a potent and specific inhibitor of Smad3 via inhibiting the effects of TGF-β1. SIS3 inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation with no effect on Smad2, p38 MAPK, ERK or PI 3-kinase signaling. It inhibits TGF-β1-induced myofibroblast differentiation of dermal fibroblasts. Group: Pharmaceutical. Alternative Names: (2E)-1-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-propenone hydrochloride. CAS No. 521984-48-5. Pack Sizes: 20 mg. Product ID: B0084-121733. Molecular formula: C28H27N3O3.HCl. Mole weight: 489.99. Custom synthesis is available. Send your inquiries for more information. | London |
| Trametinib | A MEK inhibitor that suppresses MEK1 and MEK2 with IC50 of 0.92 and 1.8 nM and no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. It has been approved by FDA, in combination with Tafilnar, for the treatment of metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation. Group: Pharmaceutical. Alternative Names: GSK-1120212; GSK 1120212; GSK1120212; JTP74057; JTP 74057; JTP-74057; Mekinist. CAS No. 871700-17-3. Pack Sizes: 500 mg. Product ID: B0084-307744. Molecular formula: C26H23FIN5O4. Mole weight: 615.39. Custom synthesis is available. Send your inquiries for more information. | London |
| Tricirbine | Triciribine is a potent AKT inhibitor and a cell-permeable tricyclic nucleoside molecule with potential antineoplastic activity. Akt-1, -2, and -3 are serine/threonine protein kinases in the phosphatidylinositol (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival. Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt-1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. Triciribine is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3. It does not inhibit phosphatidylinositol 3 (PI3)-Kinase or PDK1, the direct upstream activators of Akt, nor does it inhibit PKC, PKA, ERK1/2, serum- and glucocorticoid-inducible kinase, p38, STAT3, or JNK signalling pathways. Triciribine effectively inhibits growth of Akt-overexpressing human cancer cell lines in vitro with 50% inhibition at ~5-10 μM. It also inhibit growth of tumor xenografts in mice by greater than 80% at a dose of 1 mg/kg/day. Group: Pharmaceutical. Alternative Names: VQD-002; VQD 002; VQD002; API-2; Akt Inhibitor V; Pentaazacentopthylene; Tricyclic nucleoside; 1,5-Dihydro-5-methyl-1-beta-D-ribofuranosyl-1,4,5,6,8-pentaazaacenaphthylen-3-amine. CAS No. 35943-35-2. Pack Sizes: 100 mg. Product ID: B1370-090988. Molecular formula: C13H16N6O4. Mol | London |
| Ulixertinib | Ulixertinib, also known as VRT752271, is an inhibitor of ERK protein kinase. Group: Pharmaceutical. Alternative Names: (S)-4-(5-chloro-2-(isopropylamino)pyridin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide; BVD-523; BVD 523; BVD523; VRT752271; VRT752271; VRT 752271; Ulixertinib. CAS No. 869886-67-9. Pack Sizes: 500 mg. Product ID: B2693-460061. Molecular formula: C21H22Cl2N4O2. Mole weight: 433.333. Custom synthesis is available. Send your inquiries for more information. | London |
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