1784282-12-7
KHS101 hydrochloride
CAS: 1784282-12-7
Molecular Formula: C18H22ClN5S
1784282-12-7 - Names and Identifiers
| Name | KHS101 hydrochloride |
| Synonyms | KHS101 hydrochloride |
| CAS | 1784282-12-7 |
1784282-12-7 - Physico-chemical Properties
| Molecular Formula | C18H22ClN5S |
| Molar Mass | 375.92 |
| Solubility | Soluble in DMSO |
| Storage Condition | -20℃ |
| Use | KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3). |
| Target | TACC3 |
| In vitro study | KHS101 increases neuronal differentiation of adherently cultured rat NPCs in a dose-dependent fashion (EC 50 ~1 μM). KHS101-induced neuron formation (40-60% TuJ1+ cells at 1.5–5 μM KHS101) is also observed under neurosphere-forming conditions in secondary neurospheres derived from both the hippocampus and the subventricular zone (SVZ) of adult rats. Moreover, hippocampal NPCs treated with KHS101 and cultured adherently on microelectrode arrays for 12 d exhibit neuronal morphologies as well as spontaneous spiking activity, hence indicating the presence of functional, maturing neurons. KHS101 markedly attenuates tumor cell growth as compared to the cells treated with the vehicle [dimethyl sulfoxide (DMSO)]. TACC3 is a known target of KHS101 in rodent neural progenitor cells. KHS101 has been shown to cause cellular destabilization of TACC3, hence reducing endogenous TACC3 protein levels over time . |
| In vivo study | Tumor cell proliferation is markedly reduced in KHS101-treated tumors (about twofold). KHS101-treated tumors show signs of elevated cell death (reduced cellularity/increased pyknosis) compared with tumors treated with vehicle control. KHS101 treatment markedly reduces both frontal-to-caudal tumor expansion and corpus callosum invasion of vimentin-positive GBM1 cells. It is also found that the survival of animals carrying GBMX1 tumors (established 2 or 6 weeks before treatment) is markedly increased by the KHS101 treatment regimen for 10 weeks. None of the mice have to be removed from the study because of adverse side effects of the treatment. An additional experiment using a continuous KHS101 treatment regimen until the experimental endpoints also shows a marked increase in the survival of GBMX1-bearing animals. Histological endpoint analysis of KHS101- and vehicle-treated animals confirms a significantly decreased tumor size in KHS101-treated mice. |
1784282-12-7 - Reference
| Reference Show more | 1: Pawar V, Srivastava R. Chitosan-Polycaprolactone Blend Sponges for Management of Chronic Osteomyelitis: A Preliminary Characterization and In vitro Evaluation. Int J Pharm. 2019 Jul 22:118553. doi: 10.1016/j.ijpharm.2019.118553. [Epub ahead of print] PubMed PMID: 31344444. 2: Xu Q, Li Y, Jing Y, Lv N, Wang L, Li Y, Yu L. Epigenetic modifier gene mutations-positive AML patients with intermediate-risk karyotypes benefit from decitabine with CAG regimen. Int J Cancer. 2019 Jul 25. doi: 10.1002/ijc.32593. [Epub ahead of print] PubMed PMID: 31344264. 3: Ohno K, Zhao C, Nishina Y. Polymer-Brush-Decorated Graphene Oxide: Precision Synthesis and Liquid-Crystal Formation. Langmuir. 2019 Jul 25. doi: 10.1021/acs.langmuir.9b01747. [Epub ahead of print] PubMed PMID: 31343884. 4: deVries T, Dentiste A, Di Lea C, Pichette V, Jacobs D. Effects of Renal Impairment on the Pharmacokinetics of Once-Daily Amantadine Extended-Release Tablets. CNS Drugs. 2019 Jul 24. doi: 10.1007/s40263-019-00651-1. [Epub ahead of print] PubMed PMID: 31342404. |
1784282-12-7 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.66 ml | 13.301 ml | 26.602 ml |
| 5 mM | 0.532 ml | 2.66 ml | 5.32 ml |
| 10 mM | 0.266 ml | 1.33 ml | 2.66 ml |
| 5 mM | 0.053 ml | 0.266 ml | 0.532 ml |
Last Update：2024-01-02 23:10:35
1784282-12-7 - Cell Experiment
Rat NPCs were derived and cultured as described previously by others. After hippocampal cell isolation, the number of dissociated cells was determined and ?5 × 10^5 cells were plated in 60-mm uncoated plates. After overnight incubation (37 °C, 5% CO2, and 95% humidity), the medium was changed and the cells were expanded and maintained in an undifferentiated state on polyornithine- (10 μg/mL in water) and laminin-coated (5 μg/mL in PBS;) dishes in DMEM/F12 supplemented with N2 and basic fibroblast growth factor (bFGF, 20 ng/mL;). For KHS101 and shRNA-induction experiments, early passage cells (passaged no more than six times after hippocampal isolation) were trypsinized and plated at a density of ?1,000 cells/cm2 into N2 medium (DMEM/F12 supplemented with N2) containing KHS analogs (e.g., KHS101, KHS92, and NP; SI Text) at different concentrations (0.5–5 μM) or DMSO (0.1%), RA (1–2 μM), BDNF (100 ng/mL), and/or BMP4 (50–100 ng/mL) for 4 d .
Last Update：2023-08-16 21:32:38
1784282-12-7 - Animal Experiment
To investigate the pharmacokinetic properties of KHS101, male Sprague–Dawley rats were administered 3 mg/kg KHS101 i.v. or s.c. One rat was killed per time point at 5 min, 40 min, 1 h, and 3 h after dosing, and samples of blood (100 μL) and whole brains were collected. In a separate study, rats were administered 6 mg/kg KHS101 i.v. or s.c. Five blood samples of 100 μL each were collected serially via a jugular vein catheter at 2 min (i.v. only), 0.5 h (s.c. only), and 1, 3, 7 and 24 h after dosing. Plasma and homogenized whole brain samples were analyzed by liquid chromatography-tandem mass spectrometry (LC-MS/MS). To study neuronal differentiation upon KHS101 administration in vivo, adult Fisher 344 rats (?10 wk old) received s.c. injections of 6 mg/kg KHS101 or vehicle control (5% ethanol in 15% Captisol). All rats received one daily i.p. injection of 200 mg/kg BrdU for 6 consecutive days after the first day. After 14 d, the animals were killed and perfusion fixed, and the brains were removed and subjected
Last Update：2023-08-16 21:32:38
1784282-12-7 - References
| biological activity | KHS101 is a small molecule inhibitor of TACC3, a key component of the centrosome microtubule dynamic network. |
| Target | Value |
Last Update：2024-04-09 02:00:15
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Mobile: 18021002903
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