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KHS101 hydrochloride 

Cat. No.: HY-10996A Purity: 99.85%
Handling Instructions

KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).

For research use only. We do not sell to patients.

KHS101 hydrochloride Chemical Structure

KHS101 hydrochloride Chemical Structure

CAS No. : 1784282-12-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
25 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 630 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).

IC50 & Target

TACC3[1]

In Vitro

KHS101 increases neuronal differentiation of adherently cultured rat NPCs in a dose-dependent fashion (EC50 ~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[1]. 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 [2].

In Vivo

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[2].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 160 mg/mL (425.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6601 mL 13.3007 mL 26.6014 mL
5 mM 0.5320 mL 2.6601 mL 5.3203 mL
10 mM 0.2660 mL 1.3301 mL 2.6601 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.67 mg/mL (7.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.67 mg/mL (7.10 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.67 mg/mL (7.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Rats[2]
Xenograft tumors in rats are allowed to establish for 6 weeks after injection of GBM1 cells (1×105 cells) into the forebrain striatum and treated with vehicle or KHS101 for 10 days [6 mg/kg, subcutaneously (sc), twice daily]. To examine whether the observed mitochondrial/redox anomaly is associated with reduced tumor progression, the KHS101 dosing regimen from previous neurogenesis work in rats is adapted using a 10-week tumor treatment strategy (6 mg/kg, sc, twice a day, and biweekly treatment alternating five and three treatment days per week)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

375.92

Formula

C₁₈H₂₂ClN₅S

CAS No.

1784282-12-7

SMILES

[H]Cl.CC(CNC1=NC(NCC2=CSC(C3=CC=CC=C3)=N2)=NC=C1)C

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
KHS101 hydrochloride
Cat. No.:
HY-10996A
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KHS101 hydrochloride

Cat. No.: HY-10996A