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BMS-908662
BMS-908662 is a Raf kinase inhibitor with potential antineoplastic activity. It can specifically inhibit RAF kinases, located downstream from RAS in the RAS/RAF/MEK/ERK kinase signaling pathway, which may result in reduced proliferation of tumor cells. Phase I for the treatment of Colorectal cancer and Malignant melanoma was discontinued. Uses: Colorectal cancer; malignant melanoma. Synonyms: methyl (5-(2-(5-chloro-2-methylphenyl)-1-hydroxy-3-oxoisoindolin-1-yl)-1H-benzo[d]imidazol-2-yl)carbamate;BMS908662; BMS-908662; BMS 908662; XL281; XL 281; XL-281. Grades: 98%. CAS No. 870603-16-0. Molecular formula: C24H19ClN4O4. Mole weight: 462.89.
BMS-919373
This active molecular is a Kv1.5 potassium channel inhibitor originated by Bristol-Myers Squibb. Treatment for paroxysmal atrial fibrillation is in Phase II clinical trials. Treatment for Acute coronary syndromes and Atrial fibrillation is in Phase I clinical trials. Synonyms: BMS 919373; BMS919373; 3-Pyridinesulfonamide, 5-[5-phenyl-4-[(2-pyridinylmethyl)amino]-2-quinazolinyl]-; 5-[5-Phenyl-4-[(2-pyridinylmethyl)amino]-2-quinazolinyl]-3-pyridinesulfonamide; 5-[5-phenyl-4-[[(pyridin-2-yl)methyl]amino]quinazolin-2-yl]pyridine-3-sulfonamide. Grades: 98%. CAS No. 1272353-82-8. Molecular formula: C25H20N6O2S. Mole weight: 468.54.
BMS-935177
BMS-935177 is a potent and selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 3 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. BMS-935177 inhibited calcium flux in human Ramos B cells with IC50 of 27 nM and inhibited CD69 surface expression in peripheral B cells stimulated with anti-IgM and anti-IgG. Synonyms: BMS-935177; BMS935177. Grades: ≥98%. CAS No. 1231889-53-4. Molecular formula: C31H26N4O3. Mole weight: 502.56.
BMS-936559
Anti-PD-L1 monoclonal antibody BMS-936559 binds to PD-L1, blocking its binding to and activation of its receptor programmed death 1 (PD-1), which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation. Synonyms: MDX1105; BMS936559; MDX 1105; BMS 936559; MDX-1105; BMS-936559; Anti PD L1; PD-L1 inhibitor -Bristol-Myers Squibb.
BMS-955176 TFA is the second generation HIV-1 maturation inhibitor. Synonyms: MS-955176 TFA. CAS No. 2097784-79-5. Molecular formula: C44H63F3N2O6S. Mole weight: 805.05.
BMS-983970
BMS-983970 is an oral pan-Notch inhibitor for the treatment of cancer. Synonyms: BMS-983970; BMS 983970; BMS983970. Grades: >98%. CAS No. 1584713-87-0. Molecular formula: C26H26F4N4O3. Mole weight: 518.5.
BMS-986016
BMS 986122
BMS 986122 is a positive allosteric modulator of the μ-Opioid receptor. It significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by an EC10 (30 pM) concentration of endomorphin-I in CHO-μ cells. BMS 986122 potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human recombinant μ-opioid receptors with EC50 of 8.9 μM. It also enhances [35S]GTPγ binding stimulated by the μ-opioid agonist DAMGO by 7- and 4.5-fold in C6μ glioma cell membranes. Synonyms: BMS-986122; BMS986122; 2-(3-bromo-4-methoxyphenyl)-3-[(4-chlorophenyl)sulfonyl]-thiazolidine. Grades: ≥98%. CAS No. 313669-88-4. Molecular formula: C16H15BrClNO3S2. Mole weight: 448.8.
BMS-986142
Bruton's tyrosine kinase (BTK) is a nonreceptor tyrosine kinase. It is a member of the Tec family of kinases. BTK plays an essential role in B cell receptor (BCR)-mediated signaling as well as Fcγ receptor signaling in monocytes and Fcε receptor signaling. BMS-986142 is a potent, selective and reversible BTK inhibitor with IC50 of 0.5 nM. It potently inhibits BCR-stimulated expression of CD69 on B cells in human whole blood with IC50 of 90 nM. Synonyms: BMS-986142; BMS986142. Grades: ≥98%. CAS No. 1643368-58-4. Molecular formula: C32H30F2N4O4. Mole weight: 572.60.
BMS-986158
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins with potential antineoplastic activity. Synonyms: 2-[3-(3,5-dimethyltriazol-4-yl)-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol; BMS-986158; BMS 986158; BMS986158. CAS No. 1800340-40-2. Molecular formula: C30H33N5O2. Mole weight: 495.62.
BMS 986187
BMS 986187 is a potent and selective δ-opioid receptor positive allosteric modulator (EC50 = 30 nM) exhibiting 100-fold selectivity for δ over μ-opioid receptor. Synonyms: BMS 986187; BMS986187; BMS-986187; 3,4,5,6,7,9-Hexahydro-3,3,6,6-tetramethyl-9-[4-[(2-methylphenyl)methoxy]phenyl]-1H-xanthene-1,8(2H)-dione. Grades: ≥98% by HPLC. CAS No. 684238-37-7. Molecular formula: C31H34O4. Mole weight: 470.61.
BMS 986188
BMS 986188 is a novel potent and selective positive allosteric modulator of the delta-opioid receptor. It is selective for δ- over μ-opioid receptors with EC50 of 10 μM in the presence of leu-enkephalin and the μ-opioid receptor agonist endomorphin 1, respectively. Synonyms: MS-986188; BMS 986188. Grades: ≥98%. CAS No. 1776115-10-6. Molecular formula: C30H31BrO4. Mole weight: 535.5.
BMS-986195
BMS-986195 is a Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 0.1 nM. Synonyms: Branebrutinib; BMS 986195; BMS986195. Grades: ≥98% by HPLC. CAS No. 1912445-55-6. Molecular formula: C20H23FN4O2. Mole weight: 370.42.
BMS CCR2 22
BMS CCR2 22 is a potent CCR2 antagonist. Synonyms: N-[2-[[2-[ (4-methylsulfanylbenzoyl) amino]cyclohexyl]amino]-2-oxoethyl]-2- (propan-2-ylcarbamoylamino) -5- (trifluoromethyl) benzamide. CAS No. 445479-97-0. Molecular formula: C28H34F3N5O4S. Mole weight: 593.66.
BMT-1438
BMT-1438 is a selective inhibitor of Janus kinase (JAK) family with less side effcts which is potentially used for the treatment of rheumatoid arthritis and other autoimmune diseases. It has a preference for JAK1 and JAK3. BMT-1438 showed excellent effect both in vitro and in a collagen-induced arthritis mouse model. Uses: The potential treatment of rheumatoid arthritis and other autoimmune diseases. Synonyms: BMT-1438; BMT 1438; BMT1438.
BMT-145027
BMT-145027 is a potent mGluR5 PAM without inherent agonist activity with an EC50 of 47 nM. BMT-145027 is a non-MPEP site PAM to demonstrate in vivo efficacy. Synonyms: BMT-145027; BMT 145027; BMT145027; 3-[4-chloro-3-(trifluoromethyl)phenyl]-4-cyclopropyl-6-phenyl-2H-pyrazolo[3,4-b]pyridine-5-carbonitrile. CAS No. 2018282-44-3. Molecular formula: C23H14ClF3N4. Mole weight: 438.83.
BMY 14802 hydrochloride
BMY 14802 hydrochloride is a potent sigma receptor antagonist (IC50 = 112 nM) with weak affinity for 5-HT1A and α1 receptors. BMY 14802 is potentially used as an atypical antipsychotic agent for schizophrenia treatment. Uses: Potential atypical antipsychotic agent. Synonyms: BMY 14802 hydrochloride; BMS-181100 hydrochloride; BMY14802 hydrochloride; BMS181100 hydrochloride; BMY-14802 hydrochloride; BMS 181100 hydrochloride; BMY 14802 HCl; α-(4-Fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol hydrochloride. Grades: ≥98% by HPLC. CAS No. 105565-55-7. Molecular formula: C18H22F2N4O.HCl. Mole weight: 384.86.
BNC-105
BNC105 is a novel compound being developed by Bionomics as a Vascular Disrupting Agent (VDA) for treatment of cancer. VDAs are drugs that disrupt the blood vessels that nourish tumours. BNC105 acts as a tubulin polymerization inhibitor and displays 80-fold higher potency against endothelial cells than that of CA4P. CA4P is a VDA currently under evaluation in phase III clinical trials. BNC105 is more potent and offers a wider therapeutic window. CA4P produces 90% vascular disruption at its no observed adverse event level (NOAEL), whereas BNC105 causes 95% vascular disruption at 1/8th of its NOAEL. Tissue distribution analysis of BNC105 in tumor-bearing mice showed that while the drug is cleared from all tissues 24 hours after administration, it is still present at high concentrations within the solid tumor mass. Furthermore, BNC105 treatment causes tumor regressions with complete tumor clearance in 20% of treated animals. Synonyms: BCN-105; BCN105; BCN 105. CAS No. 945771-74-4. Molecular formula: C20H20O7. Mole weight: 372.373.
Bnlm
Bnlm is a Grp94 selective inhibitors. Grades: >98%. CAS No. 1380296-82-1. Molecular formula: C20H19ClN2O2. Mole weight: 386.83.
BNTX maleate
BNTX maleate is a selective DOR (δ1 opioid receptor) antagonist with Ki of 0.83 nM (rat). It inhibits neurogenic ion transport in porcine ileal mucosa. Synonyms: 7-Benzylidenenaltrexone maleate. Grades: ≥99%. CAS No. 864461-31-4. Molecular formula: C27H27NO4·C4H4O4. Mole weight: 545.59.
BO3482
BO3482, a dithiocarbamate carbapenem, inhibits the growth of methicillin-resistant Staphylococci (MRS) (MIC90= 6.25 mg/mL) and has a dithiocarbamate chain at the C-2 position of 1beta-methyl-carbapenem. Synonyms: BO3482; BO 3482; BO-3482; (4R, 5S, 6S)-6-[ (1R)-1-hydroxyethyl]-3-[2-hydroxyethyl (methyl)carbamothioyl]sulfanyl-4-methyl-7-oxo-1-azabicyclo[3. 2. 0]hept-2-ene-2-carboxylic acid;sodium. CAS No. 198013-53-5. Molecular formula: C14H20N2NaO5S2. Mole weight: 383.44.
Boc5
Boc5, a non-peptide glucagon-like peptide-1 (GLP-1R) receptor agonist. Synonyms: 1,3-Bis[[4-(Tert-Butoxy-Carbonylamino)Benzoyl]Amino]-2,4-Bis[3-Methoxy-4-(Thiophene-2-Carbonyloxy)-Phenyl]Cyclobutane-1,3-Dicarboxylic Acid. Grades: ≥98% by HPLC. CAS No. 917569-14-3. Molecular formula: C54H52N4O16S2. Mole weight: 1077.1.
Boc-AEVD-CHO trifluoroacetate salt
Boc-AEVD-CHO is an inhibitor of caspase-8 (Ki = 1.6 nM) that also inhibits caspase-1, -3, -6, and -9 (Kis = <12, 42, 52, and 48 nM, respectively). It inhibits apoptosis induced by the aneugen nocodazole in isolated human peripheral blood mononuclear cells (PBMCs) at concentration of 300 μM. Synonyms: Boc-Ala-Glu-Val-Asp-CHO. Grades: ≥95%. Molecular formula: C22H36N4O10·xCF3COOH. Mole weight: 516.54.
Boceprevir
An NS3 serine protease inhibitor of hepatitis C virus, for the treatment of HCV infection. Synonyms: EBP 520; EBP-520; EBP520; SCH-503034; SCH503034; SCH 503034 trade name: Victrelis. Grades: 0.98. CAS No. 394730-60-0. Molecular formula: C27H45N5O5. Mole weight: 519.687.
Bohemine
Bohemine, structurally similar to Olomoucine and Roscovitine, is a 2,6,9-trisubstituted purine derivative that inhibits cyclin-dependent kinases (CDKs) and exhibits anticancer activity. Synonyms: 3-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]propan-1-ol; 6-benzylamino-2-(3-hydroxypropylamino)-9-isopropylpurine; bohemine. Grades: ≥97%. CAS No. 189232-42-6. Molecular formula: C18H24N6O. Mole weight: 340.42.
Bombinakinin-GAP
Bombinakinin-GAP is a bioactive bradykinin-related peptide that reduces 60% food intake following i.c.v. administration in rats. Synonyms: BOMBINAKININ-GAP; 573671-91-7; AKOS024457065; Bombinakinin M Gene Associated Peptide. CAS No. 573671-91-7. Molecular formula: C145H219N39O39S3. Mole weight: 3228.75.
Bombinakinin M
Bombinakinin M is a potent bradykinin receptor agonist with selectivity for mammalian arterial smooth muscle bradykinin receptors, displaying ~ 50-fold greater potency than bradykinin. Synonyms: Maximakinin. CAS No. 509151-65-9. Molecular formula: C100H159N31O24. Mole weight: 2179.55.
Bometolol Hydrochloride
Bometolol is a beta-adrenergic blocking drug. Synonyms: 5-[3-[2-(3,4-dimethoxyphenyl)ethylamino]-2-hydroxypropoxy]-8-(2-oxopropoxy)-3,4-dihydro-1H-quinolin-2-one;hydrochloride. CAS No. 65023-16-7. Molecular formula: C25H33ClN2O7. Mole weight: 508.99.
Bopindolol malonate
Bopindolol is a non-selective, potent and long-acting β-adrenergic receptor antagonist. It demonstrates inhibition of H2O2-induced lipid peroxdiation. Bopindolol malonate slowly dissociates into the active metabolites 4-(3-tert-butylamino-2-hydroxypropoxy)-2-methyl indole and 4-(3-tert-butylaminopropoxy)-2-carboxyl indole which both demonstrate potent β1-adrenoceptor blocking activity. Formulations containing bopindolol have been used to treat essential and renovascular hypertension. Uses: Adrenergic beta-antagonists. Synonyms: Bopindolol Malonate; AC1LCS45; SCHEMBL348872; CTK8F8315; HE393689; LS-120081; D01794; Wandonorm. Grades: ≥98%. CAS No. 82857-38-3. Molecular formula: C23H28N2O3·C3H4O4. Mole weight: 484.5.
Bosentan hydrate
Bosentan inhibits the presser response to big ET-1 both after i.v. and oral administration, with a long duration of action and no intrinsic agonist activity. Synonyms: Ro 47-0203; Ro 470203; Ro470203; Ro-470203. Grades: >98%. CAS No. 157212-55-0. Molecular formula: C27H29N5O6S.H2O. Mole weight: 569.63.
BP 554 maleate
BP 554 maleate is a selective 5-HT1A agonist. Synonyms: Piperazine, 1-[3-(1,3-benzodioxol-5-yloxy)propyl]-4-phenyl-, (2Z)-2-butenedioate (1:1); 1-(3-(Benzo[d][1,3]dioxol-5-yloxy)propyl)-4-phenylpiperazine maleate; 1-[3-(3,4-methylenedioxyphenoxy)propyl]-4-phenylpiperazine maleate. Grades: ≥99% by HPLC. CAS No. 1221401-95-1. Molecular formula: C20H24N2O3.C4H4O4. Mole weight: 456.48.
BPI-3016
BPI-3016 is an analogue of human glucagon-like peptide 1 (hGLP-1) that has a long effect on type 2 diabetes mellitus. In vitro, BPI-3016 exhibited an affinity to GLP receptors and promotes cAMP production. In vivo, the half-life of BPI-3016 was 95h after single dosing in pharmacokinetic studies in diabetic cynomolgus monkey models. Uses: The treatment of type 2 diabetes. Synonyms: BPI-3016; BPI 3016; BPI3016.
BPIQ-I
BPIQ-I is an extremely potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) with IC50 of 25 pM. It can inhibit the growth of SKOV3 and MDA-468 tumor cell lines with EC50 values of 6.5 and 30 μM, respectively. Uses: Protein kinase inhibitors. Synonyms: PD 159121. Grades: ≥95%. CAS No. 174709-30-9. Molecular formula: C16H12BrN5. Mole weight: 354.2.
BPIQ-II hydrochloride
BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) with IC50 of 8 pM. It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR. Synonyms: PD 158294. Grades: ≥98%. CAS No. 171179-37-6. Molecular formula: C15H10BrN5·HCl. Mole weight: 376.6.
BPO-27 racemate
BPO-27 racemate inhibited CFTR with IC50 ? 8 nM and had greatly improved in vitro metabolic stability and aqueous solubility compared to PPQ-102. Synonyms: BPO-27 (racemate); BPO 27 racemate; BPO27 racemate; BPO-27 racemate; CHEMBL1831075; CHEMBL 1831075; CHEMBL-1831075; BPO-27 racemat. CAS No. 1314873-02-3. Molecular formula: C26H18BrN3O6. Mole weight: 548.34.
BPR1J-097
BPR1J-097 is a novel potent FLT3 inhibitor with an IC50 of 11?nM. Synonyms: BPR1J097; BPR1J-097; BPR1J 097; BPR1-J097; BPR1 J097; BPR1J097. Grades: >98%. CAS No. 1327167-19-0. Molecular formula: C27H28N6O3S. Mole weight: 516.62.
BPTU
BPTU is an allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM) that binds receptors outside of the helical bundle. BPTU blocks inhibition of spontaneous contraction of rat and mouse colon, which is induced by electrical field activation, nicotine and P2Y agonists. It exhibits antithrombotic activity and reduces platelet aggregation. Uses: Antithrombotic. Synonyms: BPTU; BMS-646786; BMS 646786; BMS646786; BMS compound 16; N-[2-[2-(1,1-Dimethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoromethoxy)phenyl]urea. Grades: ≥98% by HPLC. CAS No. 870544-59-5. Molecular formula: C23H22F3N3O3. Mole weight: 445.43.
BQ 788 sodium salt
BQ 788 sodium salt is a potent, selective ETB receptor antagonist (IC50 = 1.2 nM) without significant activity on ETA receptor (IC50= 1300 nM). Uses: Antihypertensive agents. Synonyms: cis-N-[N-[N-[(2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl]-1-(methoxycarbonyl)-D-tryptophyl]-D-norleucine Monosodium Salt; N-[[(2R,6S)-2,6-Dimethyl-1-piperidinyl]carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine Monosodium Salt; N-[(cis-2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine Monosodium Salt; (R)-2-((R)-2-((S)-2-((2S,6R)-2,6-Dimethylpiperidine-1-carboxamido)-4,4-dimethylpentanamido)-3-(1-(methoxycarbonyl)-1H-indol-3-yl)propanamido)hexanoic Acid Sodium Salt. Grades: 95%. CAS No. 156161-89-6. Molecular formula: C34H50N5NaO7. Mole weight: 663.78.
BQCA
BQCA is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR), as it dose-dependently reduces the concentration of acetylcholine required to activate the M1 receptor. Uses: A highly selective positive allosteric modulator of the m1 muscarinic acetylcholine receptor (machr). Synonyms: 1-(4-Methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid; 1,4-Dihydro-1-[(4-methoxyphenyl)methyl]-4-oxo-3-quinolinecarboxylic Acid. Grades: ≥98%. CAS No. 338747-41-4. Molecular formula: C18H15NO4. Mole weight: 309.32.
Bradanicline
Bradanicline acts as a partial agonist at the α7 subtype of the neural nicotinic acetylcholine receptors. It showed cognitive enhancing effects in animal studies, and was used as a potential treatment for schizophrenia and attention deficit disorder. It was used for Alzheimer's disease and cognitive impairment, but was discontinued. It was being developed by Targacept and was in phase II trials, but now it is terminated. Uses: Bradanicline was used as a potential treatment for schizophrenia and attention deficit disorder. it was used for alzheimer's disease and cognitive impairment. Synonyms: TC-5619; TC 5619; TC5619; N-[(2S,3R)-2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]octan-3-yl]-1-benzofuran-2-carboxamide;TC-5619-023;TC5619-023. Grades: 98%. CAS No. 639489-84-2. Molecular formula: C22H23N3O2. Mole weight: 361.44.
Bradanicline hydrochloride
Bradanicline hydrochloride is Alpha-7 Nicotinic Receptor Agonist. It showed cognitive enhancing effects in animal studies, and was being developed as a potential treatment for schizophrenia and attention deficit disorder. It was discontinued for Alzheimer's disease and cognitive impairment in schizophrenia in late 2013. It was also discontinued for ADHD, and no longer seems to be being developed. Uses: Bradanicline hydrochloride was being developed as a potential treatment for schizophrenia and attention deficit disorder. Synonyms: TC-5619;TC5619;TC-5619-023;TC5619-023;N-((2S,3R)-2-(pyridin-3-ylmethyl)quinuclidin-3-yl)benzofuran-2-carboxamide hydrochloride. Grades: >98%. CAS No. 1111941-90-2. Molecular formula: C22H24ClN3O2. Mole weight: 397.90.
B-Raf IN 1
B-Raf IN 1 is a highlt potent and selective B-Raf inhibitor. It was equipotent against c-Raf. Synonyms: B-Raf-IN-1; B-Raf-IN 1; B-Raf-IN1; MDK36057; MDK-36057; MDK 36057. Grades: >98%. CAS No. 950736-05-7. Molecular formula: C29H24F3N5O. Mole weight: 515.53.
B-Raf inhibitor
aA B-Raf inhibitor, pyrazine and pyrrolo[2,3-b]pyridine derivatives, useful in the treatment of cancer and proliferative diseases. Synonyms: Benzamide, N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-[(6-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy]-. Grades: >98%. CAS No. 1315330-11-0. Molecular formula: C29H31F3N6O2. Mole weight: 552.59.
B-Raf inhibitor 1
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 μM and 2 nM for A375 proliferation and A375 p-ERK respectively. Synonyms: B-Raf Inhibitor 1; B-Raf-Inhibitor 1; B-Raf-Inhibitor-1; MDK0403; MDK-0403; MDK 0403. Grades: >98%. CAS No. 1093100-40-3. Molecular formula: C26H19ClN8. Mole weight: 478.94.
B-Raf inhibitor 1 dihydrochloride
B-Raf inhibitor 1 is an inhibitor of B-Raf kinase with IC50 values of 0.31μM and 0.72μM for cell proliferation, respectively in A375 and HCT116. B-Raf is important in signal transduction and some mutant B-Raf occurs in cancer cells. The most common mutation of these is V600E, which makes B-Raf kinase constitutively active. B-Raf inhibitor 1 belongs to the type IIA inhibitors and binds to the DFG-out ATP-binding site of B-Raf. The selectivity of B-Raf inhibitor 1 is less than of other type inhibitors. Besides mutant B-Raf, it can also inhibit wild type B-Raf and other tyrosine kinase. In cells with wild type B-Raf, B-Raf inhibitor 1 can activate the RAF-MEK-ERK signaling pathway via Raf dimerization. The preclinical toxicity test shows B-Raf inhibitor 1 can induce hyperplasia in a mouse model. Synonyms: 1,5-Isoquinolinediamine, N1-(4-chlorophenyl)-6-methyl-N5-[3-(9H-purin-6-yl)-2-pyridinyl]-, hydrochloride (1:2). Grades: >98%. CAS No. 1191385-19-9. Molecular formula: C26H21Cl3N8. Mole weight: 551.86.
Brain Natriuretic Peptide (1-32) (human) trifluoroacetate salt
Brain natriuretic peptide (BNP) (1-32) is an endogenous peptide that has cardiovascular functions and belongs to the family of natriuretic peptides. It is an agonist of natriuretic peptide receptors (NPRs) 1 and 3 with Kd values of 7.3 and 13 pM, respectively. It also binds to human recombinant NPR1 and NPR3 with IC50 values of 8 and 2.6 nM, respectively. It also relaxes contractions induced by prostaglandin F2α (PGF2α) in isolated porcine coronary artery and rat aortic strips (IC50s = 0.02 and 12.1 nM, respectively). Synonyms: BNP (1-32) (human). Grades: ≥95%. Molecular formula: C143H244N50O42S4·xCF3COOH. Mole weight: 3464.04.
BRD3308 is a highly selective HDAC3 inhibitor with IC50 of 54 nM. BRD3308 inhibits pancreatic β-cell apoptosis induced by inflammatory cytokines or glycolipid toxic stress, and increases the release of functional insulin. BRD3308 activates HIV-1 transcription and destroys the HIV-1 incubation period. Synonyms: 4-Acetylamino-N-(2-Amino-4-Fluorophenyl)-Benzamide; CHEMBL4293858; SCHEMBL15551809; BDBM178100. Grades: 98%. CAS No. 1550053-02-5. Molecular formula: C15H14FN3O2. Mole weight: 287.29.
BRD4770
BRD4770 is a novel histone methyltransferase inhibitor. BRD4770 reduced cellular levels of di- and trimethylated H3K9 without inducing apoptosis, induced senescence, and inhibited both anchorage-dependent and -independent proliferation in the pancreatic cancer cell line PANC-1. ATM-pathway activation, caused by either genetic or small-molecule inhibition of G9a, may mediate BRD4770-induced cell senescence. BRD4770 may be a useful tool to study G9a and its role in senescence and cancer cell biology. Synonyms: BRD4770; BRD-4770; BRD 4770. Grades: 0.98. CAS No. 1374601-40-7. Molecular formula: C25H23N3O3. Mole weight: 413.477.
BRD4884
BRD4884 is a selective HDAC inhibitor with IC50 values of 29 nM, 62 nM, and 1.09 μM for HDAC1, 2, and 3. It possesses preferential binding kinetics with seven-fold longer half-life. BRD4884 crosses the blood brain barrier and has been evaluated in CK-p25 mice, a mouse model of neurodegeneration. It acts by enhancing the learning and memory processes. Synonyms: BRD-4884; BRD 4884. Grades: ≥98%. CAS No. 1404559-91-6. Molecular formula: C18H19FN2O2. Mole weight: 314.4.
BRD6688
BRD6688 is an HDAC inhibitor with IC50 values of 21 nM, 100 nM, and 11.48 μM for HDAC1, 2, and 3, respectively. It possesses preferential binding kinetics with six-fold extended half-life on HDAC2 compared to HDAC1. It crosses the blood brain barrier and has been shown to rescue the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model of neurodegeneration. Synonyms: BRD-6688; BRD 6688. Grades: ≥98%. CAS No. 1404562-17-9. Molecular formula: C16H18N4O. Mole weight: 282.3.
BRD 6989
BRD 6989 is a small molecule inhibitor with high selectivity for CDK8 over CDK19. It is an analog of the natural product cortistatin A (dCA), which inhibits CDK8 and upregulates IL-10. BRD 6989 selectively binds a complex of CDK8 with an IC50 of 200 nM. It also inhibits IFNγ-induced phosphorylation of STAT1 at Ser 727 site in BMDCs. It may be useful for inflammatory disorders. Synonyms: 2-Amino-5,6,7,8-tetrahydro-6-methyl-4-(3-pyridinyl)-3-quinolinecarbonitrile; BRD-6989; BRD6989. Grades: ≥98%. CAS No. 642008-81-9. Molecular formula: C16H16N4. Mole weight: 264.33.
BRD73954
BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively. Synonyms: BRD73954; BRD-73954; BRD 73954. Grades: >98%. CAS No. 1440209-96-0. Molecular formula: C16H16N2O3. Mole weight: 284.31.
BRD9539
BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2) with an IC50 value of 6.3 μM. It is selective for G9a and PRC2 over SU39H1 and NDMT1 up to a concentration of 40 μM. BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration. Synonyms: BRD-9539; BRD 9539. Grades: ≥98%. CAS No. 1374601-41-8. Molecular formula: C24H21N3O3. Mole weight: 399.4.
BRD 9757
BRD9757 is a potent and selective histone deacetylases 6 (HDAC6) inhibitor with IC50 of 30 nM. It displays selectivity for HDAC6 over Class I HDACS (>20-fold) and Class II HDACs (>400-fold). Synonyms: N-Hydroxy-1-cyclopentene-1-carboxamide; BRD9757; BRD-9757. Grades: ≥98%. CAS No. 1423058-85-8. Molecular formula: C6H9NO2. Mole weight: 127.14.
BRD 9876
BRD 9876 is an ATP non-competitive kinesin Eg5 inhibitor. It selectively inhibits microtubule-bound Eg5 leading to an arrest in G2/M phase. Synonyms: BRD9876; BRD-9876; BRD 9876; 6-(1,1-Dimethylethyl)-2,3-naphthalenedicarbonitrile; 6-Tert-Butyl-2,3-naphthalenedicarbonitrile. Grades: ≥99% by HPLC. CAS No. 32703-82-5. Molecular formula: C16H14N2. Mole weight: 234.3.
Brecanavir
Brecanavir is a tyrosyl-based arylsulfonamide, high-affinity, protease inhibitor (PI) for the treatment of human immunodeficiency virus type-1. This compound potently inhibited HIV-1 in cell culture assays with 50% effective concentrations (EC(50)s) of 0.2 to 0.53 nM and was equally active against HIV strains utilizing either the CXCR4 or CCR5 coreceptor, as was found with other PIs. Brecanavir had a <5-fold increase in EC(50)s against 80% of patient isolates tested and had a greater mean in vitro potency than amprenavir, indinavir, lopinavir, atazanavir, tipranavir, and darunavir. Uses: Hiv-1 protease inhibitor. Synonyms: Brecanavir; UNII-E367I8C7FI; CHEMBL206031; GW-0385; GW-640385; GW-640385X; VX-385; GW0385; GW640385; GW640385X; VX385; GW 0385; GW 640385; GW 640385X; VX 385; [(3aS,4R,6aR)-2,3,3a,4,5,6a-hexahydrofuro[2,3-b]furan-4-yl] N-[(2S,3R)-4-[1,3-benzodioxol-5-ylsulfonyl(2-methylpropyl)amino]-3-hydroxy-1-[4-[(2-methyl-1,3-thiazol-4-yl)methoxy]phenyl]butan-2-yl]carbamate. Grades: ≥98%. CAS No. 313682-08-5. Molecular formula: C33H41N3O10S2. Mole weight: 703.82.
Brilliant Blue G
Brilliant Blue G is a dye which is commonly used in laboratories to stain or quantify proteins. It can act as a selective inhibitor of the P2X purinoceptor channel P2X7 (IC50s = 10.1 and 265 nM for rat and human P2X7, respectively). A variety of methods have been developed for using Brilliant Blue G to stain gels with ease and sensitivity. Synonyms: Acid Blue 90; CBBG; Coomassie Brilliant Blue G-250; NSC 328382. Grades: ≥98%. CAS No. 6104-58-1. Molecular formula: C47H48N3O7S2·Na. Mole weight: 832.04.
BRL 15572
BRL-15,572 is selective 5-HT1D antagonist with around 60x selectivity over other related receptors. It is a useful tool for the differentiation between human 5-HT1B and 5-HT1D receptors in functional studies. Uses: Serotonin 5-ht1 receptor antagonists. Synonyms: RL 15572; RL15572; RL-15572; 1-(Diphenylmethyl)-2-(4-(3-chlorophenyl)-1-piperazinyl)ethanol;193611-72-2 (HCl). Grades: 98%. CAS No. 734517-40-9. Molecular formula: C25H27ClN2O. Mole weight: 406.95.
BRL-15572 dihydrochloride
BRL-15572 displays high affinity and selectivity for h5-HT1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D than 5-HT1B receptors. Uses: Serotonin 5-ht1 receptor antagonists. Synonyms: BRL-15572; BRL 15572; BRL15572. Grades: >98%. CAS No. 193611-72-2. Molecular formula: C25H27ClN2O.2HCl. Mole weight: 479.87.
BRL 15572 hydrochloride
BRL 15572 hydrochloride is a selective h5-HT1D antagonist with 60-fold selectivity over h5-HT1B. Synonyms: BRL 15572 hydrochloride; BRL15572 hydrochloride; BRL-15572 hydrochloride; 3-[4-(4-Chlorophenyl)piperazin-1-yl]-1,1-diphenyl-2-propanol hydrochloride. CAS No. 1173022-77-9. Molecular formula: C25H27ClN2O.HCl. Mole weight: 443.42.
BRL-37344 sodium
BRL37344 is a selective β3-adrenergic receptor agonist originated by GlaxoSmithKline. Ki value is 287nM for β3 receptor, 1750nM for β1 receptor and 1120nM for β2 receptor. BRL37344 can decrease nerve-evoked contractions in human detrusor smooth muscle isolated strips, it can also stimulate fuel oxidation by soleus muscle in vitro. BRL37344 increases glucose transport into L6 myocytes through a mechanism different from that of insulin. But preclinical for Diabetes mellitus was discontinued. Uses: Diabetes mellitus. Synonyms: BRL-37344 sodium; BRL 37344 sodium; BRL37344 sodium; sodium; 2- [4- [ (2R) -2- [ [ (2R) -2- (3-chlorophenyl) -2-hydroxyethyl] amino] propyl] phenoxy] acetate. Grades: 98 %. CAS No. 127299-93-8. Molecular formula: C19H21ClNNaO4. Mole weight: 385.82.
BRL44385
BRL44385, a novel guanine analogue, is a potent and selective inhibitor of herpes simplex virus types 1 and 2 and varicella zoster virus. Synonyms: 2-amino-9-(3-hydroxypropoxy)-3H-purin-6-one; 9-(3-hydroxypropoxy)guanine; BRL 44385; BRL-44385. Grades: >98%. CAS No. 114778-60-8. Molecular formula: C8H11N5O3. Mole weight: 225.2.
BRL 50481
BRL 50481 is a potent, selective substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (Ki = 180 nM). Uses: A pde7 inhibitor that has acceptable selectivity for in vivo studies. Synonyms: BRL-50481; BRL 50481; BRL50481. 3-(N,N-Dimethylsulfonamido)-4-methylnitrobenzene, 5-Nitro-2-N,N-trimethylbenzenesulfonamide. Grades: ≥95%. CAS No. 433695-36-4. Molecular formula: C9H12N2O4S. Mole weight: 244.27.
BRL 52537 hydrochloride
BRL 52537 hydrochloride is a potent and highly selective KOR-1 (κ-opioid receptor) and MOR (μ-opioid receptor) agonist with analgesic effects. Synonyms: BRL52537 hydrochloride; BRL-52537 hydrochloride; (±)-1-(3,4-Dichlorophenyl)acetyl-2-(1-pyrrolidinyl)methylpiperidine hydrochloride; Ethanone, 2-(3,4-dichlorophenyl)-1-[2-(1-pyrrolidinylmethyl)-1-piperidinyl]-, hydrochloride (1:1); Piperidine, 1-[(3,4-dichlorophenyl)acetyl]-2-(1-pyrrolidinylmethyl)-, monohydrochloride; Piperidine, 1-[(3,4-dichlorophenyl)acetyl]-2-(1-pyrrolidinylmethyl)-, monohydrochloride, (±)-; BRL 52537 monohydrochloride. Grades: ≥98% by HPLC. CAS No. 112282-24-3. Molecular formula: C18H24Cl2N2O.HCl. Mole weight: 391.77.
BRL-54443
BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. Synonyms: BRL54443; BRL-54443; BRL 54443. Grades: >98%. CAS No. 57477-39-1. Molecular formula: C14H18N2O. Mole weight: 230.31.
BRN-103
BRN-103 can suppress the phosphorylation of vascular endothelial growth factor (VEGF) receptor 2. It can also inhibit the activations of AKT and eNOS. These results show that BRN-103 inhibits VEGF-mediated angiogenesis signaling in human endothelial cells. Synonyms: BRN103; BRN103; BRN 103; 2-((1-benzylpiperidin-4-yl)amino)-N-(3-chlorophenyl)nicotinamide. Grades: 98%. CAS No. 1346265-80-2. Molecular formula: C24H25ClN4O. Mole weight: 420.93.
Brofaromine Hydrochloride
Brofaromine Hydrochloride is a reversible inhibitor of monoamine oxidase A(RIMA). It acts on norepinephrine, epinephrine, serotonin and dopamine. It was mainly used in the treatment of depression and anxiety. It was developed by Novartis and was in clinic phase 3, but now it was terminated. Uses: Brofaromine hydrochloride was mainly used in the treatment of depression and anxiety. Synonyms: CGP-11305A HCl;CGP11305A HCl;Brofaromine HCl;4-(7-Bromo-5-methoxy-2-benzofuranyl)piperidine hydrochloride;Piperidine, 4-(7-bromo-5-methoxy-2-benzofuranyl)-, monohydrochloride. Grades: 98%. CAS No. 63638-90-4. Molecular formula: C14H17BrClNO2. Mole weight: 346.65.
Brombuterol
Brombuterol is found to be a novel β-adrenergic agonist that can increase the meat-to-fat ratio but it is banned in animal feeds. Synonyms: 1-(4-Amino-3,5-dibromophenyl)-2-tert-butylaminoethanol. CAS No. 41937-02-4. Molecular formula: C12H18Br2N2O. Mole weight: 366.097.