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Bisindolylmaleimide VIII acetate
Bisindolylmaleimide VIII (BIM VIII) is a selective protein kinase C (PKC) inhibitor with IC50 of 158 nM for rat brain that acts at the ATP binding site. Bis VIII has been previously shown to enhance Fas-mediated apoptosis through a protein kinase C-independent mechanism. BIM VIII does not inhibit the tyrosine phosphorylation or the activation of phospholipase C γ1. BIM VIII inhibits carbachol-evoked noradrenaline release from human SH-SY5Y neuroblastoma cells with an IC50 of 600 nM. Synonyms: BIM VIII; Ro 31-7549. Grades: ≥98%. CAS No. 138516-31-1. Molecular formula: C24H22N4O2·C2H4O2. Mole weight: 458.5.
Bisindolylmaleimide X hydrochloride
Bisindolylmaleimide X hydrochloride is a potent and selective cell-permeable protein kinase C (PKC) inhibitor with IC50 of 15 nM for rat brain PKC. It has also been identified as an inhibitor of Cdk2 with IC50 of 200. It has been used to activate mesenchymal stem cells, which increases the surface expression of homing ligands that bind to intercellular adhesion molecule and target delivery of these cells to sites of inflammation. Uses: Enzyme inhibitors. Synonyms: BIM X; Ro 31-8425. Grades: ≥98%. CAS No. 145317-11-9. Molecular formula: C26H24N4O2·HCl. Mole weight: 461.
Bisindolylmaleimide XI hydrochloride
Bisindolylmaleimide XI hydrochloride is a cell-permeable selective inhibitor of PKC displaying a 10-fold greater selectivity for PKCα with IC50 of 9.3 nM. It is a 4-fold greater selectivity for PKC-βI over PKCε with IC50 of 108 nM. It prevents T cell-driven chronic inflammatory responses in several rat models. Synonyms: BIM XI; Ro 31-0432. Grades: ≥98%. CAS No. 145333-02-4. Molecular formula: C28H28N4O2·HCl. Mole weight: 489.
Bithionol sulfoxide
Bithionol sulfoxide is a clinically approved anti-parasitic drug. It has been shown to inhibit solid tumor growth in several preclinical cancer models. Synonyms: Bitin-S. Grades: >98%. CAS No. 844-26-8. Molecular formula: C12H6Cl4O3S. Mole weight: 372.05.
BIX
BIX is a BiP (Hsp70-5) ER chaperone inducer that induces BiP expression in vitro and in vivo. BIX protects against ER-stress induced cell death in neuronal and retinal cell lines, and also protects against ischaemia-induced hippocampal cell death in vivo. Synonyms: 2-(3,4-Dihydroxyphenyl)-2-oxoethyl ester thiocyanic acid; Thiocyanic acid,2-(3,4-dihydroxyphenyl)-2-oxoethyl ester. Grades: ≥98% by HPLC. CAS No. 101714-41-4. Molecular formula: C9H7NO3S. Mole weight: 209.22.
BIX-01294
BIX-01294, a diazepin-quinazolinamine derivative, is a selective inhibitor of G9a histone methyl transferase (G9a HMTase) that impairs G9a HMTase and generation of H3K9me2 in vitro. It does not compete with cofactor S-adenosyl-methionine. It enhances reprogramming efficiency of neural progenitor cells to the same levels as when four transcription factors (Oct4, Klf4, Sox2 and c-Myc) were introduced to somatic cells for generation of induced pluripotent stem cells. It may replace the requirement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS). Synonyms: BIX-01294; BIX 01294; BIX01294. Grades: >98%. CAS No. 935693-62-2. Molecular formula: C28H38N6O2. Mole weight: 490.64.
BIX01294 hydrochloride hydrate
Histone methyltransferases (HMT) are histone-modifying enzymes (e.g., histone-lysine N-methyltransferases and histone-arginine N-methyltransferases) that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. BIX 01294 is a diazepin-quinazolinamine derivate and G9a histone methyltransferase inhibitor with IC50 of 1.9 μM and GLP inhibitor with IC50 of 0.7 μM. It less effectively inhibits the HMTase G9a-like protein and has no effect on other known HMTases. BIX 01294 was reported to function by blocking the histone binding sites. It modulates the epigenetic status of chromatin and has been used to improve the reprogramming efficiency of iPSC generation. Synonyms: BIX 01294; BIX-01294. Grades: ≥98%. CAS No. 1808255-64-2. Molecular formula: C28H38N6O2·3HCl·xH2O. Mole weight: 600.
BIX-02188
BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM. Synonyms: BIX02188; BIX-02188; BIX 02188. CAS No. 334949-59-6. Molecular formula: C25H24N4O2. Mole weight: 412.493.
BL 1249
BL 1249 is a putative potassium channel activator and acts as a K2P2.1 (TREK-1) channel opener. It exhibits selectivity for bladder over vascular tissue in vitro and in vivo (EC50= 1.26 and 21.0 μM for cultured bladder and aortic tissues, respectively). Synonyms: BL1249; BL 1249; BL-1249; 5,6,7,8-Tetrahydro-N-[2-(2H-tetrazol-5-yl)phenyl]-1-naphthalenamine; N-[2-(2H-tetrazol-5-yl)phenyl]-5,6,7,8-tetrahydronaphthalen-1-amine. Grades: ≥99% by HPLC. CAS No. 18200-13-0. Molecular formula: C17H17N5. Mole weight: 291.35.
(+)-Blebbistatin
(+)-Blebbistatin is the inactive enantiomer of Blebbistatin, an inhibitor of myosin II ATPase. (+)-Blebbistatin can be used as a negative control of the active enatiomer (-)-Blebbistatin. Synonyms: (R)-(+)-Blebbistatin; (3aR)-(+)-1,2,3,3a-Tetrahydro-3a-hydroxy-6-methyl-1-phenyl-4H-pyrrolo[2,3-b]quinolin-4-one. Grades: ≥99% by HPLC. CAS No. 1177356-70-5. Molecular formula: C18H16N2O2. Mole weight: 292.34.
(±)-Blebbistatin
(±)-Blebbistatin is a selective inhibitor of myosin II ATPase. It reversibly blocks cell blebbing, and disrupts directed cell migration and cytokinesis in vertebrate cells; inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly. Synonyms: Blebbistatin; (±)-1,2,3,3a-Tetrahydro-3a-hydroxy-6-methyl-1-phenyl-4H-pyrrolo[2,3-b]quinolin-4-one. Grades: ≥98% by HPLC. CAS No. 674289-55-5. Molecular formula: C18H16N2O2. Mole weight: 292.34.
BM152054
BM152054, a thiazolidinedione, revealed to be potent PPARg-activators in transient transfection assays in vitro. Synonyms: BM152054; BM 152054; BM-152054; 5-[[4-[2-(5-methyl-2-thiophen-2-yl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl]methyl]-1,3-thiazolidine-2,4-dione; BM 15.2054; BM-15.2054; BM15.2054. CAS No. 213411-84-8. Molecular formula: C22H18N2O4S3. Mole weight: 470.58.
BM-212
BM-212, a piperazine derivative, has been found to be effective in restraining the mycobacteria and exhibit intracellular bactericidal activity at some extent. Uses: Anti-bacterial agents. Synonyms: BM-212; BM 212; BM212. UNII-U9HSU4GZWL; BM212; 1-[[1,5-bis(4-chlorophenyl)-2-methylpyrrol-3-yl]methyl]-4-methylpiperazine; 1-{[1,5-Bis(4-chlorophenyl)-2-methylpyrrol-3-yl]methyl}-4-methylpiperazine; U9HSU4GZWL. Grades: 98%. CAS No. 146204-42-4. Molecular formula: C23H25Cl2N3. Mole weight: 414.37.
BML-210
BML-210 is a Histone deacetylase (HDAC) inhibitor (IC50 = 87 μM), inducingchanges in gene expression profile. Uses: A histone deacetylase (hdac) inhibitor. Synonyms: BML-210; BML 210; BML210; CAY10433; CAY-10433; CAY 10433N1-(2-aminophenyl)-N8-phenyloctanediamide; N-(2-aminophenyl)-N'-phenyl-octanediamide. Grades: ≥98%. CAS No. 537034-17-6. Molecular formula: C20H25N3O2. Mole weight: 339.43.
BML-278
BML-278 is a selective Sirt1 activator (EC150 = 1μM) structurally based on a dihydropyridine scaffold. It has much weaker effects on Sirt2 and Sirt3. BML-278 is active in whole cells and arrests cell cycle at G1/S phase in U937 cells. It has much weaker effects on Sirt2 and Sirt3. BML-278 is active in whole cells and arrests cell cycle at G1/S phase in U937 cells. Synonyms: BML 278; BML278. Grades: ≥95%. CAS No. 120533-76-8. Molecular formula: C24H25NO4. Mole weight: 391.5.
BMN-673 8R,9S
BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity. PARP inhibitor BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and is activated by single-strand DNA breaks. BMN-673 has been proven to be highly active in mouse models of human cancer and also appears to be more selectively cytotoxic with a longer half-life and better bioavailability as compared to other compounds in development. Synonyms: Talazoparib (8R,9S); (8R,9S)-BMN-673; BMN673 (8R,9S); BMN 673 (8R,9S). Grades: >98%. CAS No. 1207456-00-5. Molecular formula: C19H14F2N6O. Mole weight: 380.35.
BMS-180048
BMS-180048, also know as Avitriptan Fumarate, has been found to be a5HT-1B/1D-receptor agonist that was once studied as an anti-migraine agent. Synonyms: Avitriptan Fumarate; BMS 180048; BMS-180048; BMS180048; UNII-2G25KE3954; 3-(3-(4--(5-methoxy-4-pyrimidinyl)-1-piperazinyl)propyl)-N-methyl-1H-indole-5-methanesulfonamide fumarate. Grades: 98%. CAS No. 171171-42-9. Molecular formula: C26H34N6O7S. Mole weight: 574.65.
BMS 180448
BMS 180448 is a prototype mitochondrial ATP-sensitive K+ channel stimulant. The cardioprotective effects of BMS-180448 against I/R heart injury may result from direct activation of mitoK(ATP) channel in cardiomyocytes. In Sep 2003, Phase-II for Myocardial ischaemia in USA was discontinued. Uses: Myocardial ischaemia. Synonyms: BMS 180448; BMS-180448; BMS180448; trans-N-(4-chlorophenyl)-N'-cyano-N''-(6-cyano-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-4-yl)- Guanidine. Grades: 98%. CAS No. 144264-47-1. Molecular formula: C20H18ClN5O2. Mole weight: 395.85.
BMS 180680
BMS 180680 is antibacterial activity agent of new catechol-containing monobactam. It is a cell wall inhibitor. BMS-180680 is an active compound against many species of the family Enterobacteriaceae, with MICs at which 90% of the isolates were inhibited. In Oct 2002, Phase-II for Respiratory tract infections in USA was discontinued. Uses: Respiratory tract infections. Synonyms: BMS 180680; BMS180680; BMS-180680; SQ 84,100;(2R-(2alpha,3alpha(Z)))-3-((((1-(2-Amino-4-thiazolyl)-2-((2-methyl-4-oxo-1-sulfo-3-azetidinyl)amino)-2-oxoethylidene)amino)oxy)methyl)-6,7-dihydroxy-2-quinoxalinecarboxylic acid. Grades: 98%. CAS No. 142654-34-0. Molecular formula: C19H17N7O10S2. Mole weight: 567.51.
BMS 181101
BMS 181101, an indole derivative, has been found to be a 5-HT receptor agonist that could be probably effective against depression and also restrain serotonin reuptake at some extent. It has already been discontinued by Bristol-Myers Squibb. Synonyms: BMS 181101; BMS181101; BMS-181101; AC1L42ZR; SCHEMBL4356376; DTXSID40163380; 5-fluoro-3-[3-[4-(5-methoxypyrimidin-4-yl)piperazin-1-yl]propyl]-1H-indole Dihydrochloride. Grades: 98%. CAS No. 146479-45-0. Molecular formula: C20H26Cl2FN5O. Mole weight: 442.36.
BMS 182874
BMS 182874 is an endothelin receptor antagonist used as an antihypertensive agent. Uses: Antihypertensive agents. Synonyms: 5-Ddins; BMS 182874; BMS-182874; BMS182874; CHEMBL267458; 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide. CAS No. 153042-42-3. Molecular formula: C17H19N3O3S. Mole weight: 345.417.
BMS 182874 Hydrochloride
This active molecular is a selective non-peptide Endothelin ETA receptor antagonist. It displays more than 1000-fold selectivity over ETB receptors (Ki of 48 nM for ETA receptors and >50 μM for ETB). BMS 182874 displays ET-1 inhibitory efficacy in vivo and vitro and it also inhibits ET-1-induced longitudinal muscle contraction in vitro. In 2006, BMS 182874 for coronary disorders and hypertension were discontinued in USA. Uses: Coronary disorders and hypertension. Synonyms: BMS 182874; BMS-182874; BMS182874; BMS 182874 HCl; BMS 182874 hydrochloride; 5-(dimethylamino)-N-(3,4-dimethylisoxazol-5-yl)naphthalene-1-sulfonamide hydrochloride. Grades: 98%. CAS No. 1215703-04-0. Molecular formula: C17H20ClN3O3S. Mole weight: 381.88.
BMS 183920
BMS 183920, a quinoline derivative, has been found to be an angiotensin II receptor antagonist that could have potential usage in antihypertensive study. Uses: Angiotensin ii type 1 receptor blockers. Synonyms: BMS 183920; BMS-183920; BMS183920; CHEMBL305365; 2-Cyclopropyl-3-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)oxy)-4-quinolinecarboxylic acid; 4-Quinolinecarboxylicacid, 2-cyclopropyl-3-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]oxy]-. Grades: 98%. CAS No. 153072-33-4. Molecular formula: C26H19N5O3. Mole weight: 449.47.
BMS-187308
BMS-187308, a sulfonamide derivative, has been found to be an endothelin-A (ETA) antagonist that was once studied about its activity against pressor effect in rats. Synonyms: BMS-187308; BMS 187308; BMS187308; UNII-7K0YU35900; CHEMBL106684; 7K0YU35900; SCHEMBL6767698; BDBM50068674; 2-[2-amino-4-(2-methylpropyl)phenyl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)benzenesulfonamide. Grades: 98%. CAS No. 153624-15-8. Molecular formula: C21H25N3O3S. Mole weight: 399.51.
BMS 191011
BMS 191011 is a potent opener of the large-conductance, Ca2+-activated potassium (maxi-K) channel. It is neuroprotectant in two distinct animal models of stroke (MCAO in the SHR rat and a normotensive model of focal stroke). Synonyms: 3-[(5-chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-one; BMS-191011; BMS 191011; BMS191011; UNII-LW7MXS978N; Bms-a. Grades: >99 %. CAS No. 202821-81-6. Molecular formula: C16H10ClF3N3O3. Mole weight: 370.71.
BMS-193884
BMS-193884, an oxazol derivative, has been found to be an endothelin A receptor antagonist and was once studied in the treatmen of heart failure. Uses: Endothelin receptor antagonists. Synonyms: BMS-193884; BMS 193884; BMS193884; 7ON53PV45J; SCHEMBL4204130; BDBM50091105; N-(3,4-dimethyl-1,2-oxazol-5-yl)-2-[4-(1,3-oxazol-2-yl)phenyl]benzenesulfonamide. Grades: 98%. CAS No. 176960-47-7. Molecular formula: C20H17N3O4S. Mole weight: 395.43.
BMS-193885
BMS-193885 is a potent and selective neuropeptide Y1 receptor antagonist with IC50=5.9nM, Ki=3.3 nM. BMS-193885 displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. Synonyms: dimethyl 4-[3-[3-[4-(3-methoxyphenyl)piperidin-1-yl]propylcarbamoylamino]phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate; BMS 193885; 679839-66-8BMS-193885; BMS193885; BMS 193885. Grades: >98%. CAS No. 186185-03-5. Molecular formula: C33H42N4O6. Mole weight: 590.71.
BMS-194449
BMS-194449 was found to be a β-adrenergic receptor agonist that was once studied in antihyperglycaemics as well as obesity therapy. Synonyms: BMS-194449; BMS 194449; BMS194449; UNII-93ZDV2P17I; CHEMBL320915; 93ZDV2P17I; SCHEMBL7042103; BDBM50106794; (R) -N- (5- (2- ( (bis (4- (difluoromethoxy) phenyl) methyl) amino) -1-hydroxyethyl) -2-hydroxyphenyl) methanesulfonamide. Grades: 98%. CAS No. 170686-12-1. Molecular formula: C24H24F4N2O6S. Mole weight: 544.52.
BMS-196085
BMS-196085, a sulfanilamide derivative, has been found to be a β-adrenergic receptor agonist that was once studied in obesity as well as yype 2 diabetes mellitus. Synonyms: BMS-196085; BMS 196085; BMS196085; CHEMBL322862; FM0D5L3W03; SCHEMBL7042488; BDBM50106829; UNII-FM0D5L3W03; N-[5-[(1R)-2-[[(1R)-1-[4-(difluoromethoxy)phenyl]-2-phenylethyl]amino]-1-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide. Grades: 98%. CAS No. 170686-10-9. Molecular formula: C24H26F2N2O5S. Mole weight: 492.54.
(±)-BMS 204352
(±)-BMS 204352 is a potassium channel opener that can be used in the study of buspirone metabolites for treating movement disorders. Synonyms: 3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)indolin-2-one; (+/-)-BMS 204352; (+/-)-BMS204352; (+/-)-BMS-204352. Grades: 98%. CAS No. 183720-28-7. Molecular formula: C16H10ClF4NO2. Mole weight: 359.7.
BMS-214662 hydrochloride
BMS-214662, a nonsedating benzodiazepine derivative, inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction. Treatment with BMS-214662 may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. BMS-214662 may be a useful drug for treating B-CLL and, in particular, an alternative for the therapy of purine analog-resistant or relapsed B-CLL. Synonyms: (3R)-3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-thiophen-2-ylsulfonyl-3,5-dihydro-2H-1,4-benzodiazepine-7-carbonitrile; 7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine; ARQ171; ARQ 171; ARQ-171; BMS214662; BMS214662; BMS-214662. Grades: >98%. CAS No. 195981-08-9. Molecular formula: C25H24ClN5O2S2. Mole weight: 526.1.
BMS-229724
BMS-229724 is a selective tight-binding inhibitor of cytosolic phospholipase A2 (cPLA2) in that it did not inhibit secreted phospholipase A2 in vitro, nor phospholipase C and phospholipase D in cells. BMS-22972 acts at the lipid/water interface and possesses anti-inflammatory activity in skin inflammation models. Synonyms: 4-[4-[2-[2-[bis (4-chlorophenyl) methoxy]ethylsulfonyl]ethoxy]phenyl]-1, 1, 1-trifluorobutan-2-one; 4- (4- (2- (2- (bis (4-chlorophenyl) methoxy) ethylsulfonyl) ethoxy) phenyl) -1, 1, 1-trifluoro-2-butanone; BMS-229724; BMS 229724; BMS229724; 42AD6D8ECA; SCHEMBL3304414; LS-46643; UNII-42AD6D8ECA. Grades: >98%. CAS No. 221914-85-8. Molecular formula: C27H25Cl2F3O5S. Mole weight: 589.45.
BMS-248360
BMS-248360 is a first orally active generation dual action receptor antagonist. BMS-248360 antagonized both Ang II AT1 and endothelin ETA receptors (AT1 IC50=8.5, ETA IC50=8.9 nM). Synonyms: 2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-[(3,3-dimethyl-2-oxopyrrolidin-1-yl)methyl]phenyl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)benzenesulfonamide; BMS-248360; BMS 248360; BMS248360; UNII-EEP77N970Y; CHEMBL11706; EEP77N970Y; SCHEMBL4764273; BDBM50117910. Grades: >98%. CAS No. 254737-87-6. Molecular formula: C36H45N5O5S. Mole weight: 659.84.
BMS-265246
BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM. It is 25-fold more selective for CDK1/2 than CDK4. Synonyms: BMS265246; BMS-265246; BMS 265246. Grades: >98%. CAS No. 582315-72-8. Molecular formula: C18H17F2N3O2. Mole weight: 345.34.
BMS 299897, under the IUPAC name 4-[2-[(1R)-1-(N-(4-chlorophenyl)sulfonyl-2,5-difluoroanilino)ethyl]-5-fluorophenyl]butanoic acid, synthesized by the radiosynthesis group at Bristol-Myers Squibb, is a β-secretase inhibitor that has the potential for treatment of Alzheimer's diseases (IC50 = 12 nM; gamma-secretase express: EC50 = 7 nM (CHO cells)). BMS 299897 blocks the formation of Aβ40 (IC50 = 7.9 nM) and Aβ42 (IC50 = 7.9 nM) in the brain, and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Synonyms: 4-[2-[(1R)-1-(N-(4-chlorophenyl)sulfonyl-2,5-difluoroanilino)ethyl]-5-fluorophenyl]butanoic acid; 4-(2-((1R)-1-(((4-chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid; BMS299897; BMS 299897; BMS-299897; 290315-45-6; 2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl]-5-fluoro-benzenebutanoic acid; C24H21ClF3NO4S; CHEMBL247471; SCHEMBL6394108; DTXSID50460039; 3496AH; ZINC28883606; AKOS024457319; CCG-222540; CS-1339; NCGC00346875-01; HY-50883; KB-75603; DB-017854; W-5550; BRD-K02950022-001-01-1; 2-[(1R)-1-[[(4-chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl]-5-fluoroBenzenebutanoic acid; BMS 299897|2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl-5-fluorobenzenebutanoic acid. CAS No. 290315-45-6. Molecular formula: C24H21ClF3NO4S. Mole weight: 511.94.
BMS-344577
BMS-344577 is aroylguanidine-based lactam derivative, which is a potent FXa inhibitor (FXa IC(50)=4 nM, EC(2xPT)=7 microM). Uses: Aroylguanidine-based factor xa inhibitor. Synonyms: BMS-344577; BMS344577; BMS 344577; UNII-U259PQB19A; CHEMBL570867; U259PQB19A; BDBM35316; BDBM50328724; N5-[[[(3S)-Hexahydro-2-oxo-1-[2-oxo-2-(1-pyrrolidinyl)ethyl]-1H-azepin-3-yl]imino][(2-methyl-5-benzofuranyl)amino]methyl]-N2,N2-dimethyl-2,5-pyridinedicarboxamide;(S,E)-N2,N2-dimethyl-N5-(N'-(2-methylbenzofuran-5-yl)-N-(2-oxo-1-(2-oxo-2-(pyrrolidin-1-yl)ethyl)azepan-3-yl)carbamimidoyl)pyridine-2,5-dicarboxamide. Grades: ≥95%. CAS No. 288079-93-6. Molecular formula: C31H37N7O5. Mole weight: 587.67.
BMS-345541
BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively. Synonyms: BMS-345541 free base; BMS345541; UNII-26SU0NEF5F; BMS 345541; BMS-345541. Grades: >98%. CAS No. 445430-58-0. Molecular formula: C14H17N5. Mole weight: 255.32.
BMS 345541 trifluoroacetate salt
BMS 345541 is a cell-permeable inhibitor of the IκB kinases IKKα with IC50s of 4 uM and IKKβ with IC50s of 0.3 μM, which binds at allosteric site of the enzyme and displays ~10-fold greater selectivity at IKK-2 over IKK-1. It exhibits no effect against a panel of 15 other kinases. BMS 345541 is used to explore novel roles for IKK phosphorylation and NF-κB signaling. Synonyms: IKK Inhibitor III. Grades: ≥98%. CAS No. 547757-23-3. Molecular formula: C14H17N5·2CF3COOH. Mole weight: 483.4.
BMS-347070
BMS-347070 is a COX-2 inhibitor, initially developed for the treatment for Colorectal cancer. Synonyms: (3Z) -3-[ (4-bromophenyl) - (4-methylsulfonylphenyl) methylidene]oxolan-2-one; BMS-347070; BMS 347070; BMS347070; UNII-0CKM4H090C; 0CKM4H090C; SCHEMBL6882900; SCHEMBL6882905. Grades: >98%. CAS No. 197438-73-6. Molecular formula: C18H15BrO4S. Mole weight: 407.28.
BMS-354326
BMS-354326 is a tryptase inhibitor with IC50 value of 1.8 nM. It has excellent selectivity against trypsin and most other related serine proteases. Synonyms: BMS-354326; BMS 354326; BMS354326; CHEMBL306448; BDBM50144532.(2S,3R)-4-oxo-1-((4-(1-oxo-6-phenylhexyl)-1-piperazinyl)carbonyl)-3-(2-(3-piperidinyl)ethyl)- 2-Azetidinecarboxylic acid. Grades: 98%. CAS No. 708258-16-6. Molecular formula: C28H40N4O5. Mole weight: 512.65.
BMS-378806
BMS-378806 selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus. Synonyms: BMS-378806; BMS 378806; BMS378806; BMS-806; BMS806; Bms 806. Grades: >98%. CAS No. 357263-13-9. Molecular formula: C22H22N4O4. Mole weight: 406.43.
BMS-433796
BMS-433796 is a γ-secretase inhibitor. Chronic dosing of BMS-433796 in Tg2576 mice suggested a narrow therapeutic window and Notch-mediated toxicity at higher doses. Uses: Gamma secretase inhibitors and modulators. Synonyms: BMS433796; BMS-433796; BMS 433796. (2S)-2-[[(2S)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]amino]-N-[(5S)-3-methyl-4-oxo-5H-2,3-benzodiazepin-5-yl]propanamide; BMS-433796; UNII-R1E8M783K2; 935525-13-6; CHEMBL247361; R1E8M783K2; ZINC28899741; (alphaS)-N-[(1S)-2-[[(5S)-4,5-Dihydro-3-methyl-4-oxo-3H-2,3-benzodiazepin-5-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide; (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide; Benzeneacetamide, N-((1S)-2-(((5S)-4,5-dihydro-3-methyl-4-oxo-3H-2,3-benzodiazepin-5-yl)amino)-1-methyl-2-oxoethyl)-3,5-difluoro-alpha-hydroxy-, (alphaS)-. CAS No. 935525-13-6. Molecular formula: C21H20F2N4O4. Mole weight: 430.15.
BMS 453
BMS 453 is a synthetic retinoid that acts as an RARβ agonist in vivo, and also an RARα and RARγ antagonist in vitro. It inhibits the proliferation of breast cells by inducing active transforming growth factor β (TGFβ) and causes G1 arrest. Synonyms: BMS453; BMS 453; BMS-453; BMS 189453; BMS-189453; BMS189453. 4-[(1E)-2-(5,6-Dihydro-5,5-dimethyl-8-phenyl-2-naphthalenyl)ethenyl]-benzoic acid. Grades: ≥98% by HPLC. CAS No. 166977-43-1. Molecular formula: C27H24O2. Mole weight: 380.48.
BMS 470539 dihydrochloride
BMS 470539 dihydrochloride is a potent and selective melanocortin MC1 receptor agonist (IC50 = 120 nM) with anti-inflammatory activity. It also inhibits leukocyte trafficking. Synonyms: BMS 470539 dihydrochloride; BMS470539 dihydrochloride; BMS-470539 dihydrochloride; 1-[1-(3-Methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidinyl]-1-butanone dihydrochloride. Grades: ≥98% by HPLC. Molecular formula: C32H41N5O4.2HCl. Mole weight: 632.62.
BMS-488043
BMS-488043 is a small-molecule HIV fusion inhibitor. Uses: Hiv fusion inhibitor. Synonyms: BMS-488043; BMS488043; BMS 488043; UNII-MKS21EJ435; CHEMBL238103; BMS 043; 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione. Grades: ≥98%. CAS No. 452296-83-2. Molecular formula: C22H22N4O5. Mole weight: 422.44.
BMS-509744
BMS-509744 is a selective Itk inhibitor. It is useful for treatment of inflammatory and autoimmune diseases. Synonyms: BMS-509744; BMS 509744; BMS509744; CHEMBL209148. Grades: >98%. CAS No. 439575-02-7. Molecular formula: C32H41N5O4S2. Mole weight: 623.83.
BMS-536924
BMS-536924 is a potent small molecule inhibitor of IGF-IR, which shows antitumor activity in multiple tumor models, including sarcoma. Synonyms: BMS536924; BMS-536924; BMS 536924. Grades: 0.98. CAS No. 468740-43-4. Molecular formula: C25H26ClN5O3. Mole weight: 479.965.
BMS-538203
BMS-538203 is a highly efficient HIV integrase inhibitor and antiviral agent. Synonyms: BMS-538203; BMS 538203; BMS538203. Grades: >98%. CAS No. 543730-41-2. Molecular formula: C12H12FNO5. Mole weight: 269.23.
BMS-564929
BMS-564929 is a novel androgen receptor (AR) modulator (Ki= 2.11 nM) which has been advanced to clinical trials for the treatment of age-related functional decline. Uses: Androgen receptor (ar) modulator. Synonyms: BMS-564929; BMS 564929; BMS564929. 4-[(7R,7aS)-7-hydroxy-1,3-dioxo-5,6,7,7a-tetrahydropyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrile. Grades: ≥98%. CAS No. 627530-84-1. Molecular formula: C14H12ClN3O3. Mole weight: 305.71.
BMS582949
BMS582949 is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor with IC50 value of 13nM, which plays a crucial role in regulating the biosynthesis of many inflammatory cytokines including TNFα and IL-1&beta. It is used for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers Squibb and was in clinic phase 2 trials, but now it is terminated. Uses: Bms582949 is used for the treatment of rheumatoid arthritis. Synonyms: 4-[[5-[(Cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide;BMS-582949;PS-540446; BMS 582949; PS 540446; BMS582949; PS540446. Grades: 98%. CAS No. 623152-17-0. Molecular formula: C22H26N6O2. Mole weight: 406.49.
BMS-582949 hydrochloride
BMS-582949 hydrochloride is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor with IC50 of 13 nM. It displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases including serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. It is a weak inhibitor of CYP3A4, with an IC50 value ranging from 18 to 40 μM based in multiple tests. It does not significantly inhibit cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 in vitro. It exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively. It is currently under Phase II clinical trials for the treatment of inflammatory diseases. Uses: Bms-582949 hydrochloride is used for the treatment of inflammatory diseases. Synonyms: BMS 582949 hydrochloride; BMS582949 hydrochloride; BMS-582949 hydrochloride; 4-((5-((Cyclopropylamino)carbonyl)-2-methylphenyl)amino)-5-methyl-n-propylpyrrolo(2,1-f)(1,2,4)triazine-6-carboxamide. Grades: >98%. CAS No. 912806-16-7. Molecular formula: C22H27ClN6O2. Mole weight: 442.94.
BMS585248
BMS585248 is a highly potent and novel human immunodeficiency virus type 1 (HIV-1) attachment inhibitor with 4-fluoro-6-azaindole core heterocycles. It targets the viral envelope protein gp120. It showed much improved in vitro potency and pharmacokinetic properties than the previous clinical candidate BMS488043. Uses: Bms585248 targets the viral envelope protein gp120. Synonyms: BMS-585248; BMS 585248; BMS585248; UNII-CIO2TZZ9H1; CIO2TZZ9H1; CHEMBL236995; SCHEMBL2628937;1,2-Ethanedione, 1-(4-benzoyl-1-piperazinyl)-2-(4-fluoro-7-(1H-1,2,3-triazol-1-yl)-1H-pyrrolo(2,3-c)pyridin-3-yl)-;1-(4-Benzoylpiperazin-1-yl)-2-[4-fluoro-7-(triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]ethane-1,2-dione. Grades: 98%. CAS No. 619331-12-3. Molecular formula: C22H18FN7O3. Mole weight: 447.43.
BMS 599626 dihydrochloride
BMS 599626 dihydrochloride is a potent and selective EGFR and ErbB2 inhibitor (IC50 = 22 nM and 32 nM, respectively), and also inhibits HER4 (IC50 = 190 nM). BMS 599626 displays 100-fold selectivity for EGFR and ErbB2 over VEGFR2, c-Kit, Lck, MET etc MEK and Lck. It can be used as an antiproliferative agent in vitro and anti-tumorigenic agent in vivo. Synonyms: BMS599626 dihydrochloride; BMS-599626 dihydrochloride; AC480 dihydrochloride; AC 480 dihydrochloride; AC-480 dihydrochloride; (3S)-3-Morpholinylmethyl-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamate dihydrochloride; Carbamic acid, N-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-, (3S)-3-morpholinylmethyl ester, hydrochloride (1:2); (3S)-3-Morpholinylmethyl (4-{[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino}-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbamate dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1781932-33-9. Molecular formula: C27H27FN8O3.2HCl. Mole weight: 603.48.
BMS-599626 Hydrochloride
BMS-599626 Hydrochloride is a selective and efficacious orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases with potential antineoplastic activity. It inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. Synonyms: AC480 hydrochloride; AC 480 hydrochloride; AC-480 hydrochloride; BMS-599626 HCl; BMS-599626 monohydrochloride; BMS 599626 Hydrochloride; BMS599626 hydrochloride; Carbamic acid, N-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-, (3S)-3-morpholinylmethyl ester, hydrochloride (1:1); Carbamic acid, [4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-, (3S)-3-morpholinylmethyl ester, monohydrochloride; (S)-Morpholin-3-ylmethyl (4-((1-(3-fluorobenzyl)-1H-indazol-5-yl)imino)-5-methyl-1,4-dihydropyrrolo[2,1-f][1,2,4]triazin-6-yl)carbamate hydrochloride. Grades: >98%. CAS No. 873837-23-1. Molecular formula: C27H28ClFN8O3. Mole weight: 567.01.
BMS 605541
BMS 605541 is a potent and ATP-competitive VEGFR-2 inhibitor (IC50 = 23 nM) displaying >10-fold selectivity for VEGFR-2 over VEGFR-1. It exhibits antitumor activity in human lung and colon tumor xenograft models. Synonyms: BMS-605541; BMS 605541; BMS605541. N-Cyclopropyl-2,4-difluoro-5-[[[2-(2-pyridinylamino)-5-thiazolyl]methyl]amino]benzamide. Grades: ≥98% by HPLC. CAS No. 639858-32-5. Molecular formula: C19H17F2N5OS. Mole weight: 401.43.
BMS-626529
BMS-626529 is a member of the new drug class of HIV-1 attachment inhibitors currently in development. BMS-663068 is the phosphonooxymethyl prodrug of BMS-626529, a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells. The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. Research result suggest that BMS-626529 should be active against the majority of HIV-1 viruses and support the continued clinical development of the compound. Synonyms: BMS626529; BMS 626529; BMS-626529; Temsavir. Grades: 99.46%. CAS No. 701213-36-7. Molecular formula: C24H23N7O4. Mole weight: 473.493.
BMS-663068 Tris
BMS-663068 tris is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection. Synonyms: Fostemsavir Tris; Fostemsavir tromethamine; BMS-663068 Tris; BMS 663068 Tris; BMS663068 Tris. Grades: >98%. CAS No. 864953-39-9. Molecular formula: C29H37N8O11P. Mole weight: 704.62.
BMS-690514 is a potent inhibitor of human epidermal growth factor receptor (HER) 1 (EGFR), 2, and 4, and vascular endothelial growth factor receptors (VEGFR) 1-3. BMS-690514 is currently under investigation as an oral agent for the treatment of solid tumors. The preclinical ADME properties of BMS-690514 suggest good oral bioavailability in humans and metabolism by multiple pathways including oxidation and glucuronidation. Synonyms: BMS-6690514; BMS 6690514; BMS6690514. Grades: 0.98. CAS No. 859853-30-8. Molecular formula: C19H24N6O2. Mole weight: 368.441.
BMS-687453
BMS-687453 is a potent and selective peroxisome proliferator activated receptor PPARα agonist. with an IC50 of 10 nM for human PPARalpha and approximately 410-fold selectivity vs human PPARgamma in PPAR-GAL4 transactivation assays. Synonyms: BMS-687453; BMS 687453; BMS687453. Grades: 98%. CAS No. 1000998-59-3. Molecular formula: C22H21ClN2O6. Mole weight: 444.87.
BMS695735
BMS695735 is a benzimidazole inhibitor of the insulin-like growth factor-1 receptor. It was also found to have potent CYP3A4 inhibition. It has broad spectrum in vivo antitumor activity. Uses: Bms695735 has broad spectrum antitumor activity. Synonyms: BMS-695735; BMS 695735; BMS695735; CHEMBL459729; BDBM27888; DNC008930; 2(1H)-Pyridinone, 4-((2-(4-chloro-1H-pyrazol-1-yl)ethyl)amino)-3-(5-(1-(3-fluoropropyl)-4-piperidinyl)-7-methyl-1H-benzimidazol-2-yl)-;(3Z)-4-[2-(4-chloropyrazol-1-yl)ethylamino]-3-[6-[1-(3-fluoropropyl)piperidin-4-yl]-4-methyl-1,3-dihydrobenzimidazol-2-ylidene]pyridin-2-one. Grades: 95%. CAS No. 1054315-48-8. Molecular formula: C26H31ClFN7O. Mole weight: 512.02.
BMS-707035
BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Uses: Hiv integrase inhibitors. Synonyms: BMS-707035; BMS-707035; BMS-707035. Grades: >98%. CAS No. 729607-74-3. Molecular formula: C17H19FN4O5S. Mole weight: 410.42.
BMS-740808
BMS-740808 is a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa with Ki of 0.03 nM. Synonyms: 1-(3-amino-1,2-benzoxazol-5-yl)-6-[4-[2-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]phenyl]phenyl]-3-(trifluoromethyl)-4,5-dihydropyrazolo[3,4-c]pyridin-7-one; BMS 740808; BMS-740808; BMS740808; UNII-LDD74E663F. Grades: >99%. CAS No. 280118-23-2. Molecular formula: C31H27F3N6O3. Mole weight: 588.58.
BMS 753
BMS 753 is a RARα-selective agonist (Ki = 2 nM) that modulates the ATRA-inducible cytochrome P450 26A1 (CYP26A1). Synonyms: BMS753; BMS 753; BMS-753. 4-[[(2,3-Dihydro-1,1,3,3-tetramethyl-2-oxo-1H-inden-5-yl)carbonyl]amino]benzoic acid. Grades: ≥99% by HPLC. CAS No. 215307-86-1. Molecular formula: C21H21NO4. Mole weight: 351.4.
BMS-754807
BMS-754807 is an orally bioavailable antagonist of human insulin-like growth factor type I receptor (IGF-1R) with potential antineoplastic activity. BMS-7548077 binds to IGF-1R, preventing IGF-1 ligand binding and activation of IGF-1R-mediated signaling pathways. Synonyms: BMS754807; BMS-754807; BMS 754807. Grades: 0.98. CAS No. 1001350-96-4. Molecular formula: C23H24FN9O. Mole weight: 461.505.
BMS 795311
BMS 795311 is a potent cholesteryl ester transfer protein (CETP) inhibitor (IC50 = 4 nM in an enzyme-based scintillation proximity assay) that inhibits cholesteryl ester transfer and increases HDL-C levels in vivo. Synonyms: BMS 795311; BMS795311; BMS-795311; N-[(1R)-1-[3-(Cyclopropyloxy)-4-fluorophenyl]-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide. Grades: ≥98% by HPLC. CAS No. 939390-99-5. Molecular formula: C33H23F10NO3. Mole weight: 671.52.
BMS-813160
BMS-813160 is an effective and selective CCR2/CCR5 antagonist with potential immunomodulatory and anti-tumor activities. It inhibits the activation of CCR2/CCR5 mediated signal transduction pathways, and may inhibit the inflammatory process, angiogenesis, tumor cell migration, tumor cell proliferation and invasion. Synonyms: BMS813160; BMS 813160; BMS 813160-Bio-X. CAS No. 1286279-29-5. Molecular formula: C25H40N8O2. Mole weight: 484.6.
BMS-890068
BMS-890068 is an acyclic P1 bi-cyclopropane acylsulfonamidetripeptide that can be used as hepatitis C virus (HCV) NS3 protease inhibitor. Uses: The treatment of hepatitis c. Synonyms: BMS-890068; BMS 890068; BMS890068.
BMS 903452
G-protein-coupled receptor 119 agonists can stimulate glucose-dependent insulin release by direct action in the pancreas and promote secretion of the incretin GLP-1 by action in the gastrointestinal tract. BMS-903452 is a selective G-protein-coupled receptor 119 (GRP119) agonist and it is efficacious in both acute and chronic in vivo rodent models of diabetes. Till now, no development was reported for the treatment of Type 2 diabetes mellitus using BMS-903452. Uses: Type 2 diabetes mellitus. Synonyms: BMS-903452; BMS 903452; BMS903452; 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one. Grades: 98%. CAS No. 1339944-47-6. Molecular formula: C21H19Cl2FN4O4S. Mole weight: 513.37.