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| Product | Description | |
|---|---|---|
| PDK1 inhibitor | PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent. Grades: >98%. CAS No. 1001409-50-2. Molecular formula: C28H22F2N4O4. Mole weight: 516.5. |  |
| PDK1 inhibitor 2610 | PDK1 inhibitor 2610 is an ATP-competitive and selective dual PI3K and PDPK1 inhibitor (IC50 values 34 nM and 94 nM for PDK1 and p-T308-PKB, respectively). Synonyms: PDK1 inhibitor 2610; 2108463-93-8; 853909-77-0; PDK1inhibitor2610; 2-(4-(8-(pyridin-3-ylethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)phenyl)acetonitrile hydrochloride. Grades: 99%. CAS No. 2108463-93-8. Molecular formula: C25H15N5.HCl. Mole weight: 421.88. | |
| PDK1 Inhibitor II - CAS 850717-64-5 | The PDK1 Inhibitor II, also referenced under CAS 850717-64-5, controls the biological activity of PDK1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy. |  |
| PDK1/Akt/Flt Dual Pathway Inhibitor - CAS 331253-86-2 | The PDK1/Akt/Flt Dual Pathway Inhibitor, also referenced under CAS 331253-86-2, controls the biological activity of PDK1/Akt/Flt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy. | |
| PIP3 Antagonist II, DM-PIT-1, N- ( (2-Hydroxy-5-nitrophenyl) carbamothioyl) -3, 5-dimethylbenzamide, N- ( ( (2-Hydroxy-5-nitrophenyl) amino) thioxomethyl) -3, 5-dimethyl-benzamide, Akt Inhibitor XXII, PDK1 Inhibitor VI) | A cell-permeable benzoylthiourea compound that is shown to compete against PIP3 for binding PH domains of Akt1 (IC50 >31uM), ARNO, GRP1, and P1. Effectively blocks PIP3-dependent cellular PI3K-PDK1-Akt signaling pathway activation in U87MG (25 to 100uM for 3d) and PDGF-induced Akt and GRP membrane translocation in serum-starved SUM159 cells (1h 100uM pretreatment), while being inactive against PDGF-induced Btk translocation or PMA-induced PLC-delta and TAPP1/2 translocations. Although DM-PIT-1 can be administered as a DMSO stock for effective culture treatments, incorporating DM-PIT-1 into PEG-PE mixed micelles enhances its solubility (up to 1mM) and i.v. dosing limit for more effective in vivo administrations (5% vs. 41% of control 4T1 tumor size in mice via 1mg/kg micelles-formulated or 0.4mg/kg free drug daily i.v., respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 701947-53-7. Pack Sizes: 25mg. Molecular Formula: C??H??N?O?S, Molecular Weight: 345.4. US Biological Life Sciences. |  Worldwide |
| PP1 Analog V, 2,3-DMB-PP1 (4-Amino-1-tert-butyl-3- (2, 3-dimethylbenzyl) pyrazolo[3, 4-d]pyrimidine, 1-tert-Butyl-3-(2,3-dimethylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Syk ASKA Inhibitor II, PDK1 ASKA Inhibitor) | A cell-permeable 3-MB-PP1 analog that is more effective than 3-MB-PP1 in inhibiting SykM442A S505A ASKA- (analog-sensitive kinase alleles) mediated cellular calcium flux (98% vs. 20% inhibition, respectively, by 1uM 2,3-DMB-PP1 or 3-MB-PP1) in Syk MASA-expressing DT40 cells. Also shown to selectively inhibit L159G ASKA, but not wt, PDK1-dependent GSK3&alpha Ser21 and S6 Ser235/236 phosphorylation upon IGF1 stimulation in mES cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 956026-24-7. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
| 10-DEBC hydrochloride | Selective inhibitor of Akt/PKB. Inhibits IGF-1-stimulated phosphorylation and activation of Akt (complete inhibition at 2.5uM), suppressing downstream activation of mTOR, p70 S6 kinase and S6 ribosomal protein. Shows no activity at PDK1, SGK1 or PI 3-kinase. Inhibits cell growth (IC50 ~ 2-6uM) and induces apoptosis in rhabdomyosarcoma cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 925681-41-0. Pack Sizes: 10mg, 50mg. Molecular Formula: C20H25N2OCl.HCl, Method for Determining. US Biological Life Sciences. | Worldwide |
| (2R)-Ethylpyrrolidine Hydrochloride | (2R)-Ethylpyrrolidine Hydrochloride is used as a reagent in the synthesis of 6-(4-pyrimidinyl)-1H-indazole derivatives as PDK1 kinase inhibitors useful in treatment of cancer, immune, metabolic and other kinase-mediated diseases. Also used as a reagent in the synthesis of aryloxazole derivatives as histamine H3 receptor antagonists or inverse agonists. Group: Biochemicals. Grades: Highly Purified. CAS No. 460748-80-5. Pack Sizes: 250mg, 2.5g. Molecular Formula: C6H14ClN, Molecular Weight: 135.639999999999. US Biological Life Sciences. | Worldwide |
| 3-Amino-5-nitrobenzoic Acid | 3-Amino-5-nitrobenzoic Acid was used as a reagent in the synthesis of 2-anilino-7H-pyrrolopyrimidines which may act as PDK1 inhibitors. Also used in the preparation of 3,5-bis substituted anilinopyrimidines which are inhibitors of tyrosine kinase EpHB4. Group: Biochemicals. Grades: Highly Purified. CAS No. 618-84-8. Pack Sizes: 250mg, 1g. Molecular Formula: C7H6N2O4, Molecular Weight: 182.13. US Biological Life Sciences. | Worldwide |
| 6BIO | Phosphoinositide-dependent kinase 1 (PDK1) inhibitor. Potent, reversible and ATP-competitive glycogen synthase kinase-3alpha/beta (GSK-3alpha/beta) inhibitor. JAK/STAT3 signaling inhibitor. Apoptosis inducer. Potent antiproliferative agent in malignant lymphoid cell. Group: Biochemicals. Alternative Names: (2'Z,3'E)-6-Bromoindirubin-3'-oxime. Grades: Highly Purified. CAS No. 667463-62-9. Pack Sizes: 1mg, 5mg, 25mg. Molecular Formula: C16H10BrN3O2. US Biological Life Sciences. | Worldwide |
| AR-12 Hydrochloride | OSU 03012, a Phenanthren derivative, has been found to be a PDPK1 inhibitor that could probably be an effctive antitumor agent. It is still under Phase I trail for solid-tumour. IC50: 5 μM. Synonyms: OSU-03012; AR-12; AR 12; AR12; OSU 03012; OSU03012; PDK1 inhibitor AR-12; 2-amino-N-[4-[5-phenanthren-2-yl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide. Grades: 98%. CAS No. 1471979-81-3. Molecular formula: C26H19F3N4O. Mole weight: 460.46. | |
| Bisindolylmaleimide II | Bisindolylmaleimide II is a potent and ATP-competitive inhibitor of protein kinase C (PKC) (IC50 = 0.01 μM). It also displays an antagonistic effect on nicotinic cholinergic receptors (IC50 ~ 0.03 μM for inhibition of catecholamine secretion in nicotine-stimulated PC-12 cells) and an inhibitory effect on PDK1 (IC50 = 14 μM). Synonyms: 3-(1H-Indol-3-yl)-4-[1-[2-(1-methyl-2-pyrrolidinyl)ethyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione. Grades: ≥97% by HPLC. CAS No. 137592-45-1. Molecular formula: C27H26N4O2. Mole weight: 438.52. | |
| BX-320 | BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC 50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 702676-93-5. Pack Sizes: 1 mg. Product ID: HY-10515. |  |
| BX-517 | BX-517, also known as PDK1 inhibitor2, is a cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDK1 inhibitor (IC50 = 6 nM). BX-517 also blocks activation of Akt in tumor cells with 10-fold more potent (IC50 = 0.1-1.0 μM) than its analogs tested at the highest dose tested (10 μM). Synonyms: (Z)-N-(3-(1-(1H-pyrrol-2-yl)ethylidene)-2-hydroxy-3H-indol-5-yl)carbamimidic acid; BX-517; BX 517; BX517; PDK1 inhibitor2. CAS No. 850717-64-5. Molecular formula: C15H14N4O2. Mole weight: 282.3. | |
| BX-795 | 3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including PKB, PKA, and certain isoforms of PKC. BX795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, which is 140- and 1600-fold more selective than PKA and PKC. It is also a potent and relatively specific inhibitor of TBK1 with IC50 of 6 nM and IKK? with IC50 of 41 nM. Synonyms: BX 795; BX795. Grades: ≥98%. CAS No. 702675-74-9. Molecular formula: C23H26IN7O2S. Mole weight: 591.47. | |
| BX912 | BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM; >10 fold selectivity over PKA, PKC, C-Kit, EGFR etc. Synonyms: BX912; BX 912; BX-912. Grades: 0.98. CAS No. 702674-56-4. Molecular formula: C20H23BrN8O. Mole weight: 471.363. | |
| CRT0066101 | CRT0066101 is a small-molecule protein kinase D (PKD) inhibitor that suppresses PDK1, PDK2 and PDK3 (PDK1: IC50 = 1 nM; PDK2: IC50 = 2.5 nM; PDK3: IC50 = 2 nM). Studies in vivo showed that CRT0066101 inhibited pancreatic cancer growth. Synonyms: Phenol, 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)-, hydrochloride (1:2); (R)-2-(4-((2-Aminobutyl)amino)pyrimidin-2-yl)-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride; 2-(4-{[(2R)-2-Aminobutyl]amino}pyrimidin-2-yl)-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride; CRT 0066101; CRT-0066101; CRT0066101 dihydrochloride. Grades: ≥95%. CAS No. 1883545-60-5. Molecular formula: C18H22N6O.2HCl. Mole weight: 411.33. | |
| Dicoumarol | Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 ( NQO1 ) and PDK1 with IC 50 s of 0.37 and 19.42 μM, respectively. Uses: Scientific research. Group: Natural products. Alternative Names: Dicumarol. CAS No. 66-76-2. Pack Sizes: 500 mg. Product ID: HY-N0645. | |
| GSK2334470 | GSK2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM), which does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. GSK2334470 also inhibited T-loop phosphorylation and activation of Akt. GSK2334470 will be a useful tool for delineating the roles of PDK1 in biological processes. Synonyms: GSK2334470; GSK2334470; GSK2334470. Grades: 0.98. CAS No. 1227911-45-6. Molecular formula: C25H34N8O. Mole weight: 462.602. | |
| HIF-1α-IN-4 | HIF-1α-IN-4 is a HIF-1α inhibitor with an IC 50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2826221-23-0. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-151465. | |
| JX 06 | JX 06 is a potent, selective and covalent pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitor with IC50 values of 49, 101 and 313 nM for PDK1, PDK2 and PDK3, respectively. It suppresses A549 lung cancer cell proliferation in vitro and reduces tumor volume of A549 xenografts in mice. Synonyms: JX-06; JX06; Bis(morpholinothiocarbonyl) Disulfide; 4, 4'- (Dithiodicarbonothioyl) bis[morpholine]; 4-Morpholinethiocarbonyl Disulfide; Dimorpholinethiuram Disulfide; Disulfide, bis(4-Morpholinylthioxomethyl); NSC 402538; bis(Oxydi-2,1-ethanediyl)-thiuram Disulfide. Grades: ≥98% by HPLC. CAS No. 729-46-4. Molecular formula: C10H16N2O2S4. Mole weight: 324.51. | |
| JX-06 | JX-06 is a potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitor (IC50 values are 28, 49 and 313 nM for PDK2, PDK1 and PDK3, respectively). JX06 Selectively Inhibits Pyruvate Dehydrogenase Kinase PDK1 by a Covalent Cysteine Modification. JX06, as a selective covalent inhibitor of PDK1 in cells, forms a disulfide bond with the thiol group of a conserved cysteine residue (C240) based on recognition of a hydrophobic pocket adjacent to the ATP pocket of the PDK1 enzyme. Uses: Designed for use in research and industrial production. Additional or Alternative Names: JX-06; JX 06; JX06. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 729-46-4. Molecular formula: C10H16N2O2S4. Mole weight: 324.49. Purity: >98%. IUPACName: Bis(morpholinothiocarbonyl) disulfide. Canonical SMILES: S=C(SSC(N1CCOCC1)=S)N2CCOCC2. Product ID: ACM729464. Alfa Chemistry ISO 9001:2015 Certified. Categories: JP-06. |  |
| Ku-0063794 | KU-0063794 is an inhibitor of both mTORC1 and mTORC2 with an IC50 of approximately 10 nM, but does not suppress the activity of 76 other protein kinases or seven lipid kinases, including Class 1 PI3Ks (phosphoinositide 3-kinases) at 1000-fold higher concentrations. KU-0063794 is cell permeant, suppresses activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK (ribosomal S6 kinase), an AGC kinase not regulated by mTOR. It also inhibited phosphorylation of the T-loop Thr308 residue of Akt phosphorylated by PDK1 (3-phosphoinositide-dependent protein kinase-1). It does not affect Thr308 phosphorylation in fibroblasts lacking essential mTORC2 subunits. KU-0063794 also suppressed cell growth and induced a G1-cell-cycle arrest. KU-0063794 will be useful in delineating the physiological roles of mTOR and may have utility in treatment of cancers in which this pathway is inappropriately activated. Uses: Differentiation. Synonyms: KU0063794; KU-0063794; KU 0063794; Ku0063794; Ku 0063794; Ku-0063794; KU63794; KU 63794; KU-63794; [5-[2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-4-morpholin-4-ylpyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol. Grades: 0.98. CAS No. 938440-64-3. Molecular formula: C25H31N5O4. Mole weight: 465.554. | |
| MP7 | MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 ( PDK1 ) inhibitor. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PDK1 inhibitor. CAS No. 1001409-50-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-14440. | |
| NU6102 (O6-Cyclohexylmethyl-2- (4-sulfamoylanilino) purine) | Potent CDK1/cyclin B (IC50 = 9.5nM) and CDK2/cyclin A3 (IC50 = 5.4nM) inhibitor. 1,000-fold more potent than NU2058. Selective for CDK1 and CDK2 compared to CDK4/D1 (IC50 = 1.6uM), DYRK1A (IC50 = 0.9uM), PDK1 (IC50 = 0.8uM) and ROCKII (IC50 = 0.6uM). Inhibits cell growth. Group: Biochemicals. Alternative Names: O6-Cyclohexylmethyl-2- (4-sulfamoylanilino) purine. Grades: Highly Purified. CAS No. 444722-95-6. Pack Sizes: 1mg, 5mg. Molecular Formula: C18H22N6O3S, Molecular Weight: 402.5. US Biological Life Sciences. | Worldwide |
| NVP-BAG956 | NVP-BAG956 is a potent, ATP-competitive and selective dual PI3K and PDK1 inhibitor in vitro and in vivo. It inhibits cellular AKT phosphorylation at Thr308 and blocks cell proliferation, causing arrest in G1 phase of the cell cycle. It slows tumor progression in mouse xenograft models. Synonyms: BAG-956; BAG 956; BAG956; NVP-BAG956; NVP-BAG-956; NVP-BAG 956. Grades: >98%. CAS No. 853910-02-8. Molecular formula: C28H21N5. Mole weight: 427.5. | |
| PS10 | PS10 is a novel, potent and ATP-competitive pan- PDK inhibitor, inhibits all PDK isoforms with IC 50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 ( K d = 239 nM) than for Hsp90 (K d = 47 μM) [1]. PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy [2].PDK: pyruvate dehydrogenase kinase. Uses: Scientific research. Group: Signaling pathways. CAS No. 1564265-82-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-121744. | |
| PS210 | PS210 is a potent and selective PDK1 activator with a K d of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1 , inhibiting the phosphorylation and activation of S6K [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1221962-86-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-121629. | |
| PS423 | PS423 is a prodrug of PS210, acting as a substrate-selective inhibitor of PDK1 , inhibiting the phosphorylation and activation of S6K. PS210 is a potent and selective PDK1 activator targeting the PIF binding pocket of PDK1 [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1221964-37-9. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-124060. | |
| Radicicol | Radicicol is an inhibitor of Hsp90 with an IC 50 value < 1 μM, and leads to proteasomal degradation [1]. Radicicol exhibits inhibition on PDK with IC 50 s of 230 μM ( PDK1 ) and 400 μM ( PDK3 ). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB [2]. Radicicol is also an inhibitor of fat mass and obesity-associated protein ( FTO ), with an IC 50 value of 16.04 μM [3]. Uses: Scientific research. Group: Natural products. Alternative Names: Monorden. CAS No. 12772-57-5. Pack Sizes: 1 mg; 5 mg. Product ID: HY-N6769. | |
| SH-5 (D-3-Deoxy-2-O-methyl-myo-inositol 1-[(R)-2-methoxy-3-(octadecyloxy)propyl hydrogen phosphate) | A cell-permeable inhibitor of Akt activation without affecting the activation of the upstream kinase PDK1 or other kinases downstream of Ras such as MAPK. Induces apoptosis and kills a variety of cancer cell lines containing high levels of active Akt. Group: Biochemicals. Alternative Names: D-3-Deoxy-2-O-methyl-myo-inositol 1-[(R)-2-methoxy-3-(octadecyloxy)propyl hydrogen phosphate. Grades: Highly Purified. Pack Sizes: 500ug. US Biological Life Sciences. | Worldwide |
| SH-6 (D-2,3-Dideoxy-myo-inositol 1-[(R)-2-methoxy-3-(octadecyloxy)propyl hydrogen phosphate) | A cell-permeable inhibitor of Akt activation without affecting the activation of the upstream kinase PDK1 or other kinases downstream of Ras such as MAPK. Induces apoptosis and kills a variety of cancer cell lines containing high levels of active Akt. Group: Biochemicals. Alternative Names: D-2,3-Dideoxy-myo-inositol 1-[(R)-2-methoxy-3-(octadecyloxy)propyl hydrogen phosphate. Grades: Highly Purified. Pack Sizes: 500ug. US Biological Life Sciences. | Worldwide |
| 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. Synonyms: VQD-002; VQD 002; VQD002; NSC-154020; NSC 154020; NSC154020; Triciribine; TCN-P; triciribine; Tricyclic nucleoside; Pentaazacentopthylene; API-2; Akt Inhibitor V. Grades: 99.81%. CAS No. 35943-35-2. Molecular formula: C13H16N6O4. Mole weight: 320.309. | |
| Triciribine | Cell-permeable. A synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. Group: Biochemicals. Alternative Names: 1,5-Dihydro-5-methyl-1-b-D-ribofuranosyl-1,2,5,6,8-pentaazanaphthylen-3-amine, NSC 154020. Grades: Highly Purified. CAS No. 35943-35-2. Pack Sizes: 1mg. US Biological Life Sciences. | Worldwide |
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