KHS101 hydrochloride

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

Cat. No.: HY-10996A Purity: 99.65%: Data Sheet
COA

SDS
Handling Instructions
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KHS101 hydrochloride is a selective neuronal differentiation inducer that can cross the blood-brain barrier. KHS101 hydrochloride exhibits selective cytotoxicity against glioblastoma multiforme (GBM). KHS101 hydrochloride interacts with transforming acidic coiled-coil protein (TACC3). KHS101 hydrochloride can be used in GBM research.

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

KHS101 hydrochloride Chemical Structure

CAS No. : 1784282-12-7

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of KHS101 hydrochloride:

KHS101 Get quote

1 Publications Citing Use of MCE KHS101 hydrochloride

•University of Califomia San Francisco. 2026.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

TACC3^[1]

In Vitro

KHS101 increases neuronal differentiation of adherent cultured rat NPCs in a dose-dependent manner (EC₅₀=~1 μM)^[1].
KHS101 (1.5-5 μM) induces neuronal formation in secondary neurospheres derived from adult rat hippocampus and subventricular zone (SVZ) under neurosphere formation conditions (40-60% TuJ1+ cells)^[1].
Furthermore, hippocampal NPCs treated with KHS101 and cultured adherently on microelectrode arrays for 12 days exhibited neuronal morphology and spontaneous spiking activity, thus indicating the presence of functional, mature neurons^[1].
Compared to cells treated with the vehicle [dimethyl sulfoxide (DMSO)], KHS101 significantly attenuated tumor cell growth^[2].
TACC3 is a known target of KHS101 in rodent neural progenitor cells. KHS101 has been shown to destabilize TACC3-expressing cells, thereby reducing endogenous TACC3 protein levels over time^[2].
KHS101 is a synthetic small molecule compound that can cross the BBB and selectively induce neuronal differentiation of hippocampal neural progenitor cells in vitro and in vivo^[3].

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

In Vivo

After KHS101 treatment, tumor cell proliferation was significantly reduced (approximately twofold decrease), and signs of tumor cell death increased (decreased cell density/increased nuclear condensation)^[2].
KHS101 significantly reduced the anterior-posterior extension and corpus callosum infiltration of vimentin-positive GBM1 cells. The study also found that KHS101 significantly improved the survival rate of animals carrying GBMX1 tumors^[2].
In a mouse intracranial glioblastoma (GBM) patient-derived xenograft (PDX) model, KHS101 (6 mg/kg, subcutaneous injection, twice daily) significantly reduced tumor growth, decreased tumor burden, induced metabolic abnormalities in tumor cells, inhibited tumor cell proliferation (decreased proportion of MKI67-positive cells), promoted tumor cell death, reduced tumor invasion and expansion, inhibited tumor extension from the frontal to the caudal region and contralateral hemisphere infiltration across the corpus callosum, and significantly prolonged the survival time of tumor-bearing 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: 99.65%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (244 KB) HNMR (182 KB) LCMS (94 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.