KHS101 hydrochloride

Name: KHS101 hydrochloride
Brand: MedChemExpress
SKU: HY-10996A
Rating: 4.5 (1 reviews)

Cat. No.: HY-10996A Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1784282-12-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 116	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 116	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 105	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 920	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of KHS101 hydrochloride:

KHS101 Get quote

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All FGFR Isoform Specific Products:

View All Isoforms

FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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 (1.5–5 μM) induces neuron formation (40-60% TuJ1+ cells) 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].

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

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].

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

Molecular Weight

375.92

Formula

C₁₈H₂₂ClN₅S

CAS No.

1784282-12-7

Appearance

Solid

Color

White to off-white

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.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 160 mg/mL (425.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 10 mg/mL (26.60 mM; ultrasonic and warming and heat to 60°C)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

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

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.67 mg/mL (7.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.84%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (246 KB) RP-HPLC (242 KB) MS (71 KB)

Handling Instructions (2659 KB)

References

[1]. Wurdak H, et al. A small molecule accelerates neuronal differentiation in the adult rat. Proc Natl Acad Sci U S A. 2010 Sep 21;107(38):16542-7. [Content Brief]

[2]. Polson ES, et al. KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. Sci Transl Med. 2018 Aug 15;10(454). pii: eaar2718. [Content Brief]

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

[1]. Wurdak H, et al. A small molecule accelerates neuronal differentiation in the adult rat. Proc Natl Acad Sci U S A. 2010 Sep 21;107(38):16542-7. [Content Brief]

[2]. Polson ES, et al. KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. Sci Transl Med. 2018 Aug 15;10(454). pii: eaar2718. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.6601 mL	13.3007 mL	26.6014 mL	66.5035 mL
	5 mM	0.5320 mL	2.6601 mL	5.3203 mL	13.3007 mL
	10 mM	0.2660 mL	1.3301 mL	2.6601 mL	6.6504 mL
	15 mM	0.1773 mL	0.8867 mL	1.7734 mL	4.4336 mL
	20 mM	0.1330 mL	0.6650 mL	1.3301 mL	3.3252 mL
	25 mM	0.1064 mL	0.5320 mL	1.0641 mL	2.6601 mL
DMSO	30 mM	0.0887 mL	0.4434 mL	0.8867 mL	2.2168 mL
	40 mM	0.0665 mL	0.3325 mL	0.6650 mL	1.6626 mL
	50 mM	0.0532 mL	0.2660 mL	0.5320 mL	1.3301 mL
	60 mM	0.0443 mL	0.2217 mL	0.4434 mL	1.1084 mL
	80 mM	0.0333 mL	0.1663 mL	0.3325 mL	0.8313 mL
	100 mM	0.0266 mL	0.1330 mL	0.2660 mL	0.6650 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.