17-DMAG (Alvespimycin) HCl | CAS#467214-21-7 APExBIO 貨號A2213
特點
蛋白酶(Proteases)系列商品->>17-DMAG (Alvespimycin) HCl
APExBIO Technology LLC 是一家領先的小分子抑制劑 (Small Molecule Inhibitors)/活化劑(Activators)、化合物庫( Compound Libraries)、胜肽(Peptides)、檢測試劑盒(Assay Kits)、螢光標記(Fluorescent Label)、酶(Enzymes)、修飾核苷酸(Modified Nucleotides)、mRNA 合成以及各種分子生物學工具的供應商。APExBIO提供廣泛的產品線，涵蓋 20 多個不同的研究領域，例如癌症(cancer)、免疫學(immunology)、神經科學(neurosciences)、細胞凋亡(apoptosis)和表觀遺傳學(epigenetics)等。公司總部位於美國德州休士頓USA (Houston, Texas)，致力於服務全球客戶。高度重視產品品質。所有產品均遵循嚴格的生產指南，並附有分析證書、HPLC、質譜(Mass Spectrum)和HMNR以及體外驗證(in vitro validation)。 APExBIO產品已被《Nature》、《Cell》和《Science》等眾多頂級同行評審期刊引用。>>更多APExBio商品
蛋白酶(Proteases)也稱為肽酶(peptidases)或蛋白水解酶(proteolytic enzymes)，由大量催化肽鍵水解(hydrolysis)並隨後導致蛋白質底物(protein substrates)降解為氨基酸(amino acids)的酶組成。蛋白酶(Proteases)與多種人類疾病有關，包括癌症(cancer)、神經退行性疾病(neurodegenerative disorders)、炎症性疾病(inflammatory diseases)和心血管疾病(cardiovascular diseases)。因此，許多蛋白酶抑制劑【小分子(small molecules)和蛋白質】已被鑑定為阻斷蛋白酶的活性(proteases)。蛋白酶抑制劑可以根據它們通過兩種一般機制抑制的蛋白酶類別分為不同的類型，即不可逆的“捕獲(trapping)”反應和可逆(reversible)的緊密結合反應。蛋白酶抑制劑已被用作治療蛋白酶相關疾病的診斷劑(diagnostic)或治療劑(therapeutic agents)。
17-DMAG (Alvespimycin) HCl | CAS#467214-21-7 APExBIO 貨號A2213
Product Citation+3
Hsp90 inhibitor
17-DMAG 是 Hsp90 的抑制劑，IC50 值為 62±29nM [1]。17-DMAG 可以與 Hsp90 的 ATP 結合基序結合，抑制 Hsp90 的蛋白chaperoning活性。它將導致 Hsp90 的client proteins（如 EGFR、AKT、突變 p53 和 IKK）的錯誤折疊(misfolding)和隨後的降解(degradation) 。由於腫瘤細胞中 17-DMAG 結合所需的 Hsp90 具有更特異性的conformation，並且 Hsp90 的許多client proteins有助於腫瘤細胞的生長，因此 17-DMAG 對腫瘤細胞的毒性通常比對正常細胞的毒性更大 [2]。據報導，17-DMAG 是一種抗腫瘤劑(ntitumor agent)，在體外和初始體內試驗中具有更廣泛的可利用活性和藥學上更易於處理的特徵。 17-DMAG在處理NCI 60細胞株時可影響細胞生長，平均GI50為0.053mM。 17-DMAG 的體內活性在四個黑色素瘤模型中使用 Freiburg 人類腫瘤異種移植組和兩個肺異種移植(lung xenografts)進行了測試。它表明 17-DMAG 在兩個肺異種移植物和四個黑色素瘤模型中的兩個中具有高活性，但在另外兩個 MEXF 462 和 MEXF 514 中沒有 [3]。
- Peng Zhou, Becky K.C. Chan, et al. “A Three-Way Combinatorial CRISPR Screen for Analyzing Interactions among Druggable Targets.” Cell Rep. 2020 Aug 11;32(6):108020.PMID:32783942
- Bhola PD, Ahmed E, et al. “High-throughput dynamic BH3 profiling may quickly and accurately predict effective therapies in solid tumors.” Sci Signal. 2020;13(636):eaay1451.PMID:32546544
- Katayama K, Noguchi K, et al. “Heat shock protein 90 inhibitors overcome the resistance to Fms-like tyrosine kinase 3 inhibitors in acute myeloid leukemia.” Oncotarget. 2018 Sep 28;9(76):34240-34258.PMID:30344940
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 653.21 |
| Cas No. | 467214-21-7 |
| Formula | C32H48N4O8·HCl |
| Solubility | ≥26.2 mg/mL in DMSO; insoluble in EtOH; ≥3.04 mg/mL in H2O |
| Chemical Name | [(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-21-[2-(dimethylamino)ethylamino]-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCCN(C)C)C)OC)OC(=O)N)C)C)O)OC.Cl |
| Shipping Condition | Ship with blue ice, or upon other requests. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
APExBIO台灣代理商: https://www.apexbt.com/
APExBIO提供優質的胜肽和生物分析試劑，廣泛產品線如Protease、Chromatin/Epigenetics表觀遺傳學、MAPK Signal、DNA Damege/DNA repair、細胞凋亡、腫瘤生物學、Stem cell等研究領域， 還提供定制的服務，包括多肽合成，抗體的生產和檢測的發展。產品線DNA/RNA prep kit、Drug Screening panel、Bioactive peptides、Growth factors、Biotinylation Reagents、tag peptides、amino Acids、Growth factors等。APExBIO產品質量都伴隨著證書的分析，高效液相色譜，質譜，和HMNR數據。
| A4324 | Pioglitazone HCl | 112529-15-4 | 99.35% | PPARγ agonist |
| A4325 | PF-2545920 | 1292799-56-4 | 99.90% | PDE10A inhibitor,potent and selective |
| A4326 | TAK-700 (Orteronel) | 426219-18-3 | 99.44% | Human 17,20-lyase inhibitor |
| A4327 | Tadalafil | 171596-29-5 | 99.91% | PDE5 inhibitor |
| A4328 | Rolipram | 61413-54-5 | 98.19% | PDE4-inhibitor and an anti-inflammatory agent |
| A4329 | Cilomilast | 153259-65-5 | 99.37% | Potent PDE4 inhibitor |
| A4330 | Isotretinoin | 4759-48-2 | 99.89% | Dopamine β-hydroxylase activator |
| A4331 | GSK256066 | 801312-28-7 | 98.39% | PDE4-inhibitor,selective and highly potent |
| A4332 | Nepicastat (SYN-117) HCl | 170151-24-3 | 98.14% | Dopamine-β-hydroxylase inhibitor |
| A4333 | CPI-613 | 95809-78-2 | 99.45% | PDH/α-KGDH inhibitor |
| A4334 | Avanafil | 330784-47-9 | 99.07% | PDE5 inhibitor |
| A4335 | Mildronate | 76144-81-5 | 98.33% | GBB hydroxylase inhibitor |
| A4336 | Mycophenolate Mofetil | 128794-94-5 | 99.67% | IMPDH inhibitor |
| A4337 | Cilostazol | 73963-72-1 | 99.94% | PDE3 inhibitor |
| A4338 | Rivaroxaban | 366789-02-8 | 99.91% | Factor Xa inhibitor |
| A4339 | AGI-5198 | 1355326-35-0 | 97.43% | IDH1 inhibitor against R132 mutant,selective and cell-permeable |
| A4340 | Pimobendan | 74150-27-9 | 99.25% | Selective PDE3 inhibitor.Ca2+ channel sensitizer |
| A4341 | Apixaban | 503612-47-3 | 99.87% | Factor Xa inhibitor |
| A4342 | Gimeracil | 103766-25-2 | 99.82% | Dihydropyrimidine dehydrogenase inhibitor |
| A4343 | Dyphylline | 479-18-5 | 99.84% | Pan-PDE inhibitor |
| A4344 | Ozagrel | 82571-53-7 | 99.84% | Thromboxane A2 synthetase inhibitor |
| A4345 | MK-8245 | 1030612-90-8 | 99.76% | SCD inhibitor,potent and liver-selective |
| A4346 | Aminophylline | 317-34-0 | 99.05% | Pan-PDE inhibitor |
| A4347 | Methotrexate | 59-05-2 | 99.14% | Folate antagonist,inhibits DFHR |
| A4348 | Trilostane | 13647-35-3 | 99.58% | 3β-HSD inhibitor |
| A4349 | S- (+)-Rolipram | 85416-73-5 | 99.93% | CAMP-specific PDE4 inhibitor |
| A4350 | Pralatrexate | 146464-95-1 | 98.47% | Antifolate,a folate analog |
| A4351 | PluriSIn #1 (NSC 14613) | 91396-88-2 | 99.32% | SCD1 inhibitor |
| A4352 | Anagrelide HCl | 58579-51-4 | 99.62% | Thrombocytopenic agent |
| A4353 | Pyrimethamine | 58-14-0 | 99.65% | DHFR inhibitor |
| A4354 | UK 383367 | 348622-88-8 | 98.00% | BMP-1/PCP inhibitor,potent and selective |
| A4355 | Tosedostat (CHR2797) | 238750-77-1 | 98.96% | Aminopeptidase inhibitor |
| A4356 | Varespladib (LY315920) | 172732-68-2 | 98.00% | HnsPLA inhibitor,potent and selective |
| A4357 | Dorzolamide HCl | 130693-82-2 | 99.87% | Carbonic anhydrase inhibitor |
| A4358 | U-104 | 178606-66-1 | 99.82% | CAIX inhibitor |
| A4359 | Brinzolamide | 138890-62-7 | 99.88% | CA II inhibitor |
| A4360 | Topiramate | 97240-79-4 | 100.00% | GluR5 receptor antagonist,anticonvulsant |
| A4361 | JNJ-1661010 | 681136-29-8 | 98.00% | FAAH inhibitor,potent and selective |
| A4362 | Tioxolone | 4991-65-5 | 98.67% | CAI inhibitor |
| A4363 | Fluvastatin Sodium | 93957-55-2 | 98.84% | HMG-CoA reductase inhibitor |
| A4364 | Methazolamide | 554-57-4 | 99.79% | Carbonic anhydrase inhibitor |
| A4365 | Lovastatin | 75330-75-5 | 98.58% | HMG-CoA reductase inhibitor |
| A4366 | Rasagiline Mesylate | 161735-79-1 | 99.23% | Irreversible MAO-B inhibitor |
| A4367 | Atorvastatin Calcium | 134523-03-8 | 99.76% | HMG-CoA reductase inhibitor |
| A4368 | Safinamide Mesylate | 202825-46-5 | 98.60% | MAO-B inhibitor,potent,selective and reversible |
| A4369 | Pravastatin sodium | 81131-70-6 | 98.00% | HMG-CoA reductase inhibitor,highly selective and competitive |
| A4370 | Moclobemide (Ro 111163) | 71320-77-9 | 99.85% | Reversible inhibitor of MAO-A |
| A4371 | Ferrostatin-1 (Fer-1) | 347174-05-4 | 99.75% | Ferroptosis inhibitor, erastin-induced |
| A4372 | URB597 | 546141-08-6 | 99.58% | FAAH inhibitor,potent and selective |
| A4373 | NLG919 | 1402836-58-1 | 99.79% | Potent IDO pathway inhibitor |
| A4374 | PF-3845 | 1196109-52-0 | 98.00% | FAAH ihibitor,highly potent and selective |
| A4375 | Anacetrapib (MK-0859) | 875446-37-0 | 99.76% | RhCETP/mutant CETP(C13S) inhibitor |
| A4376 | Dalcetrapib (JTT-705, RO4607381) | 211513-37-0 | 98.00% | rhCETP inhibitor |
| A4377 | Evacetrapib (LY2484595) | 1186486-62-3 | 98.83% | CETP inhibitor,potent and selective |
| A4378 | Torcetrapib | 262352-17-0 | 98.00% | CETP inhibitor |
| A4379 | Lonafarnib | 193275-84-2 | 98.00% | Ftase inhibitor,potent and selective |
| A4381 | FK866 (APO866) | 658084-64-1 | 99.58% | NAMPT inhibitor, non-competitive, highly specific |
| A4382 | A922500 | 959122-11-3 | 97.62% | DGAT-1 inhibitor |
| A4383 | Tolcapone | 134308-13-7 | 99.42% | COMT inhibitor |
| A4384 | PF-04620110 | 1109276-89-2 | 98.00% | DGAT-1 inhibitor,potent and selective |
| A4385 | Ganetespib (STA-9090) | 888216-25-9 | 99.03% | Hsp90 inhibitor,non-geldanamycin |
| A4386 | Elesclomol (STA-4783) | 488832-69-5 | 98.00% | Oxidative stress/apoptosis inducer,potent and novel |
| A4387 | VER 155008 | 1134156-31-2 | 99.72% | HSP 70 inhibitor,adenosine-derived |
| A4388 | XL-888 | 1149705-71-4 | 98.00% | Hsp90 inhibitor |
| A4390 | Pemetrexed | 150399-23-8 | 99.88% | TS, DHFR,GARFT and AICARFT inhibitor |
| A4393 | Paclitaxel (Taxol) | 33069-62-4 | 99.71% | Antineoplastic agent |
| A4394 | Docetaxel | 114977-28-5 | 98.56% | Microtubulin disassembly inhibitor |
| A4395 | 10-DAB (10-Deacetylbaccatin) | 32981-86-5 | 98.26% | Precursor of antitumor compound Palitaxel and Docetaxel |
| A4400 | BMS 299897 | 290315-45-6 | 98.00% | γ–secretase inhibitor, potent and orally active |
| A4401 | Compound W | 173550-33-9 | 98.00% | γ-secretase inhibitor |
| A4402 | Flurizan | 51543-40-9 | 99.76% | NSAID,inhibits γ-secretase activity |
| A4403 | JLK 6 | 62252-26-0 | 98.00% | γ-secretase inhibitor |
| A4404 | L-685,458 | 292632-98-5 | 99.25% | γ-secretase inhibitor |
| A4405 | MRK 560 | 677772-84-8 | 98.00% | γ-secretase inhibitor |
| A4406 | Begacestat | 769169-27-9 | 98.00% | γ-secretase inhibitor |
| A4407 | Fumagillin | 23110-15-8 | 98.00% | Antibiotic and antiangiogenic agent |
| A4408 | SC 57461A | 423169-68-0 | 98.00% | LTA4 hydrolase inhibitor,potent and selective |
| A4409 | Spinorphin | 137201-62-8 | 98.00% | P2X3 receptors against |
| A4410 | Acetyl-Calpastatin (184-210) (human) | 123714-50-1 | 98.00% | Calpain I/II inhibitor |
| A4411 | Calpeptin | 117591-20-5 | 98.00% | Ca2+-dependent protease,calpain inhibitor |
| A4412 | MDL 28170 | 88191-84-8 | 98.00% | Calpain and cathepsin B inhibitor, selective |
| A4413 | PD 150606 | 179528-45-1 | 98.00% | Non-peptide calpain inhibitor |
| A4414 | PMPA (NAALADase inhibitor) | 173039-10-6 | 98.00% | Glutamate carboxypeptidase 2 inhibitor |
| A4415 | ZJ 43 | 723331-20-2 | 98.00% | GCP II and III/NAAG peptidase/NAALADase inhibitor |
| A4416 | AZ 10417808 | 331645-84-2 | 98.00% | Caspase-3 inhibitor,selective non-peptide |
| A4417 | Ivachtin | 745046-84-8 | 98.00% | Caspase-3 inhibitor |
| A4418 | Ac-IEPD-AFC | 1135417-31-0 | 96.06% | Recognition motif for serine protease granzyme B |
| A4419 | Ac-LEHD-AFC | 210345-03-2 | ≥95.00% | Fluorogenic caspase substrate |
| A4420 | PETCM | 10129-56-3 | 98.00% | Caspase-3 activator |
| A4422 | L 006235 | 294623-49-7 | 98.00% | Cathepsin K inhibitor |
| A4424 | SID 26681509 | 958772-66-2 | 98.00% | Human cathepsin L inhibitor,potent and reversible |
| A4425 | DPPI 1c hydrochloride | 866396-34-1 | 98.00% | DPP-IV Inhibitor |
| A4426 | K 579 | 440100-64-1 | 98.00% | Dipeptidyl peptidase IV inhibitor |
| A4427 | NVP DPP 728 dihydrochloride | 247016-69-9 | 96.76% | DPP-IV inhibitor |
| A4428 | PK 44 phosphate | 1017682-65-3 | 98.00% | DPP-IV inhibitor |
| A4429 | Vialinin A | 858134-23-3 | 98.00% | USP/isopeptidase T (IsoT)/UCH-L1 DUB inhibitor |
| A4430 | Sivelestat sodium salt | 150374-95-1 | 98.00% | Leukocyte elastase inhibitor |
| A4431 | SSR 69071 | 344930-95-6 | ≥95.00% | HLE inhibitor |
| A4432 | ARP 100 | 704888-90-4 | 98.00% | Selective MMP-2 inhibitor |
| A4433 | ARP 101 | 849773-63-3 | 98.00% | MMP inhibitor,potent and selective |
| A4434 | CL 82198 hydrochloride | 307002-71-7 | 98.00% | Selective MMP-13 inhibitor |
| A4435 | CP 471474 | 210755-45-6 | 98.00% | Broad spectrum MMP inhibitor |
| A4436 | GI 254023X | 260264-93-5 | 98.00% | Selective inhibitor of ADAM10 metalloprotease |
| A4437 | ONO 4817 | 223472-31-9 | 98.00% | MMP inhibitor |
| A4438 | PD 166793 | 199850-67-4 | 98.00% | MMP inhibitor |
| A4440 | UK 356618 | 230961-08-7 | 98.00% | MMP-3 inhibitor,potent and selective |
| A4441 | UK 370106 | 230961-21-4 | 98.00% | MMP-3/MMP-12 Inhiibitor,highly selective |
| A4442 | WAY 170523 | 307002-73-9 | 98.00% | MMP-13 inhibitor,potent and selective |
| A4443 | Gliotoxin | 67-99-2 | 98.00% | 20S proteasome inhibitor |
| A4444 | BC 11 hydrobromide | 443776-49-6 | 98.00% | Selective urokinase inhibitor |
| A4445 | 4-Chlorophenylguanidine hydrochloride | 14279-91-5 | 98.00% | Urokinase inhibitor, potent and specific |
| A4446 | R18 | 211364-78-2 | 98.00% | 14.3.3 proteins Antagonist |
| A4447 | 2,3-DCPE hydrochloride | 418788-90-6 | 98.00% | Bcl-XL protein expression downregulator |
| A4448 | Actinomycin D | 50-76-0 | 98.00% | RNA polymerase inhibitor |
| A4449 | C 75 | 191282-48-1 | 98.00% | Fatty acid synthase (FAS) inhibitor |
| A4450 | CHM 1 | 154554-41-3 | 98.00% | Tubulin polymerization inhibitor |
| A4451 | Deguelin | 522-17-8 | 98.00% | Anticancer and antiviral agent |
| A4452 | Mitomycin C | 50-07-7 | 98.00% | Inhibits DNA synthesis,antibiotic and antitumor agent |
| A4453 | NSC 687852 (b-AP15) | 1009817-63-3 | 98.15% | 19S regulatory particle Inhibitor |
| A4454 | Oncrasin 1 | 75629-57-1 | 98.00% | Proapoptotic agent |
| A4455 | Piperlongumine | 20069-09-4 | 98.00% | Inducer of cell-death |
| A4456 | Plumbagin | 481-42-5 | 98.00% | Anticancer agent |
| A4457 | Streptozocin | 18883-66-4 | 98.00% | Antibiotic and antitumor agent |
| A4458 | ARRY 520 trifluoroacetate | 885060-09-3 | 98.00% | KSP inhibitor |
| A4459 | Bax channel blocker | 335165-68-9 | 98.00% | Inhibitor of Bax-mediated mitochondrial cytochrome c release |
| A4460 | Bax inhibitor peptide P5 | 579492-83-4 | 99.59% | Bax inhibitor |
| A4461 | Bax inhibitor peptide V5 | 579492-81-2 | 99.19% | Bax inhibitor |
| A4463 | BIM, Biotinylated | 99.04% | Bim peptide fragment with a biotin moiety attached | |
| A4465 | MIM1 | 509102-00-5 | 98.69% | Mcl-1 Inhibitor |
| A4466 | Muristerone A | 38778-30-2 | ≥95.00% | TRAIL- and hFasL-induced apoptosis inhibitor |
| A4467 | SU 9516 | 377090-84-1 | 98.00% | Cdk2 inhibitor |
| A4468 | Cesium chloride | 7647-17-8 | 98.00% | Potassium channel blocker |
| A4469 | DAPK Substrate Peptide | 386769-53-5 | 98.00% | Synthetic peptide substrate for DAPK |
| A4471 | GRI 977143 | 325850-81-5 | 98.00% | LPA2 receptor non-lipid agonist |
| A4472 | Mdivi 1 | 338967-87-6 | 99.52% | Selective DRP1/Dnm1 inhibitor, cell-permeable |
| A4473 | Melphalan | 148-82-3 | 98.00% | DNA alkylating agent |
| A4474 | NQDI 1 | 175026-96-7 | 98.00% | ASK1, MAP3K5 inhibitor |
| A4475 | TLQP 21 | 869988-94-3 | 98.00% | VGF-derived peptide |
| A4476 | CP 31398 dihydrochloride | 1217195-61-3 | 98.00% | p53 stabilizer |
| A4477 | Cyclic Pifithrin-α hydrobromide | 511296-88-1 | 99.34% | P53 inhibitor |
| A4478 | HLI 373 | 502137-98-6 | 98.00% | Hdm2 ubiquitin ligase (E3) inhibitor |
| A4479 | MIRA-1 | 72835-26-8 | 98.00% | Restorer of wild-type p53 conformation/cellular function |