9月
Thalidomide-Cyanine 5；Thalidomide-Cyanine 5Thalidomide-Cyanine 5 (2024/9/8)
簡介：thalidomide-cyanine 5 is a fluorescent probe for cereblon e3 ligases. binds with high affinity to ddb1-crbn. suitable for use in tr-fret.
FAM-DEALAHypYIPMDDDFQLRSF；FAM-DEALAHypYIPMDDDFQLRSFFAM-DEALAHypYIPMDDDFQLRSF (2024/9/8)
簡介：fam-dealahypyipmdddfqlrsf is a 5,6-carboxyfluorescein (fam) labeled hif-1α peptide. it binds with high affinity to von hippel-lindau (vhl) protein (kd= 3 nm). can be used to assess ligand binding to vhl in a direct fluorescence polarization (fp) displacement assay. excitation/emission maxima (λ) = 485/520 nm. this product is a longer peptide version of fam-deala-hyp-yipd.
FAM-DEALA-Hyp-YIPD；FAM-DEALA-Hyp-YIPDFAM-DEALA-Hyp-YIPD (2024/9/8)
簡介：fam-deala-hyp-yipd is a fluorescent hif-1α peptide (kd= 180-560 nm). can be used to assess vhl binding in fluorescence polarization (fp) displacement assay, and evaluate the effect of vhl binding on degradation activity. excitation maximum = 485 nm, emission maximum = 535 nm. longer peptide version, fam-dealahypyipmdddfqlrsf, also available.
BODIPY FL VH032；BODIPY FL VH032BODIPY FL VH032 (2024/9/8)
簡介：bodipy fl vh032 is a high-affinity vhl fluorescent probe (kd= 3.01 nm) with application in time-resolved fluorescence resonance energy-transfer (tr-fret) assays for high-throughput identification and characterization of vhl ligands. bodipy fl vh032 consists of a derivative of von hippel-lindau (vhl) ligand vh 032 and a fluorophore bodipy fl(with excitation peak at 504 nm and emission peak at 520 nm), joined by a polyethylene glycol (peg) 4 linker. the bodipy fl vh032 vhl tr-fret signal is stable
cisVH 298；cisVH 298cisVH 298 (2024/9/8)
簡介：cisvh 298 is a negative control for vh 298. exhibits no detectable binding of vhl.
Zuclopenthixol；珠氯噻醇cis-Clopenthixol|||Cisordinol|||(Z)-Clopenthixol；珠氯噻醇|||cis-Clopenthixol|||Cisord (2024/9/8)
簡介：zuclopenthixol (cis-clopenthixol) is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. it is an antagonist at d1 and d2 dopamine receptors.
P21d hydrochloride；P21d hydrochlorideP21d hydrochloride (2024/9/8)
簡介：p21d hydrochloride is a potent and selective breast tumor ki nase (brk) inhibitor (ic50 = 30 nm). exhibits >650-fold selectively for brk over aurora b ki nase and lck. downregulates snail protein, restores e-cadherin expression and suppresses migration in breast cancer cells. also activein vivoand orally bioavailable.
SJF 0661；SJF 0661SJF 0661 (2024/9/8)
簡介：sjf 0661 is the negative control for sjf 0628. binds braf without inducing degradation.
CG 858-Neg；CG 858-NegCG 858-Neg (2024/9/8)
簡介：negative control for cg 858
NVS PAK1 C；NVS PAK1 CNVS PAK1 C (2024/9/8)
簡介：nvs pak1 c is a negative control of nvs pak1 1, a potent and selective pak1 inhibitor.
ETP 45835 dihydrochloride；ETP 45835 dihydrochlorideETP 45835 dihydrochloride (2024/9/8)
簡介：etp 45835 dihydrochloride is a mnk2 and mnk1 inhibitor (ic50 values are 575 and 646 nm respectively). exhibits selectivity against a panel of 24 protein ki nases, including those upstream of mnk1/2.
FC 11；FC 11FC 11 (2024/9/8)
簡介：fc 11 is a highly potent focal adhesion ki nase (fak) protac?degrader (dc50 values are 40 to 370 pm depending on cell line), which is composed of the fak inhibitor pf 562217 joined by a linker to the cereblon-binding ligand pomalidomide. the effects of fc 11 are reversible upon compound wash out. fc 11 also degrades autophosphorylated fak (pfaktyr397), displaying near complete degradation after 3 hours at 100 nm in tm3 cells.
ZNL 02-096；化合物ZNL 02-096Pomalidomide-C3-adavosertib；Pomalidomide-C3-adavosertib (2024/9/8)
簡介：znl 02-096 (pomalidomide-c3-adavosertib) is a rapid and selective degrader of wee1 (ic50=3.58 nm).znl 02-096 selectively degrades wee1 at submolar concentrations without damaging plk1, a secondary target of azd 1775.znl 02-096 induces degradation of wee1 and accumulation of dna damage in molt-4 cells in vitro, in vitro in molt-4 cells, znl 02-096 induced wee1 degradation, accumulation of dna damage, cell cycle arrest in g2/m phase and apoptosis.znl 02-096 showed anti-proliferative effects in 300
ZLN 024 hydrochloride；化合物ZLN 024 hydrochlorideZLN 024 hydrochloride (2024/9/8)
簡介：zln 024 hydrochloride is an ampk allosteric activator and stimulates the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312).
Lalistat 2；化合物Lalistat 2Lalistat 2 (2024/9/8)
簡介：lalistat 2 is a selective inhibitor of lysosomal acid lipase with ic50 of 152 nm and exhibits no inhibition of human pancreatic lipase or bovine milk lipoprotein lipase (up to 10 μm).
S-Adenosyl-DL-Methionine；S-腺苷蛋氨酸Ademetionine|||S-ADENOSYL-L-METHIONINE；Ademetionine|||S-腺苷蛋氨酸|||S-AD (2024/9/8)
簡介：s-adenosyl-dl-methionine (ademetionine) is a ubiquitous methyl donor involved in a wide variety of biological reactions, including those mediated by dna and protein methyltransferases. sam reportedly ameliorates depression, pain associated with osteoarthritis and fibromyalgia, and liver toxicity.
NCT 501 hydrochloride；NCT 501 hydrochlorideNCT 501 hydrochloride (2024/9/8)
簡介：nct 501 hydrochloride is a potent and selective aldh1a1 inhibitor (ic50 = 40 nm). exhibits >1000-fold selectivity for aldh1a1 over aldh3a1, aldh1b1, aldh2, hpgd and hsd17β4. also selective over a panel of 168 gpcrs. blood-brain barrier permeable.
MS 39N；MS 39NMS 39N (2024/9/8)
簡介：ms 39n is a negative control for ms 39. binds egfr without inducing degradation.
MS 154N；MS 154NMS 154N (2024/9/8)
簡介：ms 154n is a negative control for ms 154. the compound exhibits high binding-affinity for wt and l858r-mutant egfr (kdvalues are 3 and 4.3 nm, respectively), but does not significantly induce degradation of egfr mutants.
MS 39；MS 39MS 39 (2024/9/8)
簡介：ms 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (egfr) with high efficiency, high affinity and selectivity. ms 39, conjured by gefitinib to vhl ligand via a linker, effectively induced the degradation of mutant egfr (dc50 values in hcc827(exon 19 del) and h3255 (l858r mutation) lung cancer cell lines were 5 nm and 3.3 nm, respectively). however, there was no significant effect in wild-type egfr cell lines with concentrations up to
MS 154；MS 154MS 154 (2024/9/8)
簡介：ms 154 is a potent and selective cereblon-recruiting degrader (protac?) of mutant epidermal growth factor receptor (egfr), comprising a cereblon-binding moiety joined by a linker to gefitinib(iressa). ms 154 decreases egfr protein levels, inhibits downstream signaling in and inhibits proliferation of mutant egfr-bearing lung cancer cells (dc50values are 11 and 25 nm in hcc-827 and h3255 cells, respectively; dmax> 95% at 50 nm), but not in wt-egfr-bearing ovarian and lung cancer cells lines. bioa
BOP-JF646；BOP-JF646BOP-JF646；BOP-JF646 (2024/9/8)
簡介：bop-jf646 is a fluorescent dual α9β1/α4β1 integrin inhibitor. comprises bop conjugated to janelia fluor?646. fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. excitation maximum = 655 nm; emission maximum = 672 nm.
R-BC154；R-BC154R-BC154；R-BC154 (2024/9/8)
簡介：r-bc154 is a high affinity fluorescent α4β1/α9β1 inhibitor (kdvalues are 12.7 and 38 nm, respectively); fluorescent version of bop. rapidly and preferentially mobilizes hscs and progenitorsin vivo. excitation maximum, 561 nm; emissiosn maximum, 585 nm.
K34c hydrochloride；K34c鹽酸鹽K34c hydrochloride(939769-93-4 Free base)；K34c hydrochloride(939769-93-4 F (2024/9/8)
簡介：k34c hydrochloride is an alpha5β1 integrin antagonist for glioblastoma study.
K34c；K34cK34c (2024/9/8)
簡介：k34c is a potent and selective α5β1 integrin inhibitor (ic50 = 3.1 nm). k34c inhibits cell survival and migration, inhibits p53-dependent senescence induced by temozolomide or ellipticine and promotes apoptosis in u87mg cells. k34c also prevents tgfβ-induced infiltrationin vivoand reduces cell adhesion on fibronectin.
EMD 527040 hydrochloride；EMD 527040 hydrochlorideEMD 527040 hydrochloride (2024/9/8)
簡介：emd 527040 hydrochloride is an effective integrin αvβ6 inhibitor. the ic 50 values of emd 527040 hydrochloride were 6 nm and 1.6 μm to inhibit αvβ6 binding to fibronectin and αvβ6 expression cells to fibronectin, respectively. emd 527040 hydrochloride shows antifibrotic activity in animal models of biliary fibrosis and is active in vivo.
Auraptene；橙皮油素7-geranyloxycoumarin；橙皮油內(nèi)酯|||7-geranyloxycoumarin|||橙皮油素 (2024/9/8)
簡介：auraptene is a coumarin derived from citrus plants that bears a geranyloxyl moiety at its c-7. it has anti-inflammatory, anti-carcinogenic, anti-bacterial, neuroprotective, and hepatoprotective activities. it inhibits leukocyte activation and induces phase ii enzymes during the initiation phase of carcinogenesis.1 when examined for its potential use in alzheimer´s disease treatment, auraptene was shown to inhibit β-secretase (bace1) activity with an ic50 value of 345.1 μm.
BOP-JF549；BOP-JF549BOP-JF549；BOP-JF549 (2024/9/8)
簡介：bop-jf549 is a fluorescent dual α9β1/α4β1 integrin inhibitor. comprises bop conjugated to janelia fluor? 549. fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. excitation maximum = 549 nm; emission maximum = 571 nm.
Phototrexate；PhototrexatePhototrexate (2024/9/8)
簡介：phototrexate is a photoswitchable potent inhibitor of human dihydrofolate reductase (dhfr). phototrexate is a photochromic analog of methotrexate. antifolate activity is switched on (cis-phototrexate) by uva (375 nm) light; it can be switched off (trans-phototrexate) by blue or white light and by thermal relaxation in the dark.cis-phototrexate (ic50 = 6 nm) significantly reduces the viability of hela cells compared withtrans-phototrexate (ic50 = 34 μm).
ND1-YL2；ND1-YL2ND1-YL2；ND1-YL2 (2024/9/8)
簡介：nd1-yl2 is a peptide-based protac?degrader of steroid receptor co-activator 1 (src-1; also known as nuclear receptor coactivator 1, ncoa1). nd1-yl2 is composed of a stapled peptide that binds src-1 (yl2) joined by a linker to a tetrapeptide that binds ubr box domains. upon ternary complex formation, src-1 is polyubiquitinated and subsequently degraded via the n-degron pathway. this degrader induces dose-dependent degradation of src-1 in the mda-mb-231 triple negative breast cancer cell line (dc5
MSN交談
