OTSSP167 hydrochloride (Synonyms: OTS167 hydrochloride)

Name: OTSSP167 hydrochloride
Brand: MedChemExpress
SKU: HY-15512A
Rating: 5.0 (28 reviews)

Cat. No.: HY-15512A Purity: 99.84%: FAQs
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OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC₅₀ value of 0.41 nM.

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

OTSSP167 hydrochloride Chemical Structure

CAS No. : 1431698-10-0

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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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
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Customer Review

Based on 28 publication(s) in Google Scholar

Other Forms of OTSSP167 hydrochloride:

OTSSP167 Get quote

19 Publications Citing Use of MCE OTSSP167 hydrochloride

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2019 Nov 18;9(12):87. [Abstract]; Expression of MELK and Aurora B kinase (AurB) is determined in samples from vehicle and OTSSP167-treated mice. β-actin is used as loading control.

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2018 Nov 15;24(22):5645-5657. [Abstract]; Western blot showing protein levels of MELK, PPARγ and phospho-PPARγ^S112 in JHH-DIPG-01, HSJD-DIPG-12, SF7761 and HSJD-DIPG-07 cells after 48 hours treatment with either 20 nM or 50 nM OTSSP167.

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2018 Mar;10(3). pii: e8274. [Abstract]; Validation of effects of OTS167 on phosphorylation of p90RSK and its targets. C4-2b cells are treated with vehicle or 30 nM OTS167 for the indicated times, and levels of total and phosphorylated proteins are determined by Western blot analysis. β-Actin is used as a loading control.

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: Gynecol Oncol. 2017 Apr;145(1):159-166. [Abstract]; Western blotting demonstrates that 100 nM OTSSP167 for 48 h produces marked PARP-1 cleavage in HGSOC cell lines whereas no or weak PARP-1 cleavage is observed in normal ovarian surface epithelial cells (HOSE6-3) and in the fallopian tubal cells (FT33-tag, FT190, FT237).

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Feb 14;7:42502. [Abstract]; In vitro kinase assays are performed using MPK38 immunoprecipitates, which are obtained from cell lysates of wild-type and clonal CRISPR/Cas9 ZPR9 (T252A) KI isolates, treated with (+) or without (−) OTSSP167 (1 μM, 2 h), a MPK38-specific inhibitor, in the presence of ZPR9 immunoprecipitates as the substrate. Recombinant MPK38 proteins (lower panels), which were expressed in bacterial cells, treated with (+) or without (−) OTSSP167 are also used instead of the MPK38 immunoprecipitates (upper pan

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Feb 24;12(2):e0172832. [Abstract]; OTS167 reduces proliferation and regulates MELK transcript but not protein levels in TNBC cells. The MELK 52 kDa variant is highly expressed in the TNBC cell lines but not in luminal A MCF-7.

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Dec 20;9(2):2591-2602. [Abstract]; Effects of OTSSP167 on PARP and Caspase-3 cleavages in NB cells are shown by immunoblotting assay.

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: Patent. US20160291017A1.; Mitotic MDA-MB-468 cells are treated for 30 min with vehicle or 200 nM OTSSP167, a MELK inhibitor. Lysates are used for immunoblotting.

: OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2014 May 4;13:100. [Abstract]; MELK specific inhibitor OTSSP167 suppresses cell migration and invasion. A, Immunoblotting representing MELK expression in SGC7901 cell following OTSSP167 treatment for indicated period. In the upper panel, SGC7901 cell are treated with different concentration (0, 0.1, 1 μM) of OTSSP167 for 1 h and 2 h. In the lower panel, SGC7901/vector and SGC7901/MELK cell are treated with 1 μM OTSSP167 for 2 h. C, SGC7901/vector and SGC7901/MELK cells are treated with 1 μM OTSSP167 for indicated period and

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Description

OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC₅₀ value of 0.41 nM.

IC₅₀ & Target

IC50: 0.41 nM (MELK)

In Vitro

OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC₅₀ values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively^[1].
OTSSP167 can abrogate the mitotic checkpoint, disrupt MCC and MCC-APC/C interaction in MCF7 cells. OTSSP167 causes GFP-MELK localization to cell cortex in prometaphase cells^[2].
OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC₅₀ of 0.41 nM^[3].

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

In Vivo

OTSSP167 (20 mg/kg, i.v.) results in tumor growth inhibition (TGI) of 73% in xenograft mouse model; OTSSP167 (1, 5, and 10 mg/kg, p.o.) reveals TGI of 51, 91, and 108%, respectively. OTSSP167 (20 mg/kg, p.o.) shows no tumor growth suppressive effect on PC-14 xenografts^[1].

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

Molecular Weight

523.88

Formula

C₂₅H₂₉Cl₃N₄O₂

CAS No.

1431698-10-0

Appearance

Solid

Color

Light yellow to gray

SMILES

ClC1=CC(C2=CC=C(N=CC(C(C)=O)=C3N[C@H]4CC[C@H](CN(C)C)CC4)C3=N2)=CC(Cl)=C1O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (63.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 7.14 mg/mL (13.63 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9088 mL	9.5442 mL	19.0883 mL
5 mM	0.3818 mL	1.9088 mL	3.8177 mL
10 mM	0.1909 mL	0.9544 mL	1.9088 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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: ≥ 3 mg/mL (5.73 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (5.73 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: 3 mg/mL (5.73 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 1 mg/mL (1.91 mM); Clear solution; Need ultrasonic

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, 2 years; -20°C, 1 year (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 (284 KB) SDS (252 KB)

COA (255 KB) LCMS (136 KB)

Handling Instructions (2659 KB)

References

[1]. Chung S, Suzuki H, Miyamoto T, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget. 2012 Dec 21. [Content Brief]

[2]. Ji W, et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases. PLoS One. 2016 Apr 15;11(4):e0153518. [Content Brief]

[3]. Cho YS, et al. The crystal structure of MPK38 in complex with OTSSP167, an orally administrative MELK selective inhibitor. Biochem Biophys Res Commun. 2014 Apr 25;447(1):7-11. [Content Brief]

[4]. Jurmeister S, et al. Identification of potential therapeutic targets in prostate cancer through a cross-species approach. EMBO Mol Med. 2018 Feb 5. pii: e8274. [Content Brief]

[5]. Meel MH, et al. MELK inhibition in Diffuse Intrinsic Pontine Glioma. Clin Cancer Res. 2018 Jul 30. pii: clincanres.0924.2018. [Content Brief]

Kinase Assay ^[1]	For in vitro kinase assay, MELK recombinant protein (0.4 μg) is mixed with 5 μg of each substrate in 20 μL of kinase buffer containing 30 mM Tris-HCl (pH), 10 mM DTT, 40 mM NaF, 10 mM MgCl₂, 0.1 mM EGTA with 50 μM cold-ATP and 10 Ci of [γ-³²P]ATP for 30 min at 30°C. The reaction Is terminated by addition of SDS sample buffer and boiled for 5 min prior to SDS-PAGE. The gel is dried and autoradiographed with intensifying screens at room temperature. OTSSP167 (final concentration of 10 nM) is dissolved in DMSO and added to kinase buffer before the incubation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	In vitro cell viability is measured by the colorimetric assay using Cell Counting Kit-8. Cells are plated in 100 μL in 96-well plates at a density that generates continual linear growth (A549, 1×10³ cells; T47D, 3×10³ cells; DU4475, 4×10³ cells; 22Rv1, 6×10³ cells; and HT1197, 2×10³ cells, in 100 μL per well). The cells are allowed to adhere overnight before exposure to OTSSP167 for 72 hours at 37°C. Plates are read using a spectrophotometer at a wavelength of 450 nm. All assays are carried out in triplicate. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	MDA-MB-231 cells are injected into the mammary fat pads of NOD.CB17-Prkdc^scid/J mice. A549, MIAPaCa-2 and PC-14 cells (1×10⁵ cells) are injected subcutaneously in the left flank of female BALB/cSLC-nu/nu mice. DU145 cells are injected subcutaneously in the left flank of male BALB/cSLC-nu/nu mice. When MDA-MB-231, A549, DU145, MIAPaCa-2, and PC-14 xenografts has reached an average volume of 100, 210, 110, 250, and 250 mm³, respectively, animals are randomized into groups of 6 mice (except for PC-14, for which groups of 3 mice are used). For oral administration, OTSSP167 and other compounds are prepared in a vehicle of 0.5% methylcellulose and given by oral garbage at the indicated dose and schedule. For intravenous administration, compounds are formulated in 5% glucose and injected into the tail vein. An administration volume of 10 mL per kg of body weight is used for both administration routes. Tumor volumes are determined every other day using a caliper. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Chung S, Suzuki H, Miyamoto T, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget. 2012 Dec 21. [Content Brief] [2]. Ji W, et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases. PLoS One. 2016 Apr 15;11(4):e0153518. [Content Brief] [3]. Cho YS, et al. The crystal structure of MPK38 in complex with OTSSP167, an orally administrative MELK selective inhibitor. Biochem Biophys Res Commun. 2014 Apr 25;447(1):7-11. [Content Brief] [4]. Jurmeister S, et al. Identification of potential therapeutic targets in prostate cancer through a cross-species approach. EMBO Mol Med. 2018 Feb 5. pii: e8274. [Content Brief] [5]. Meel MH, et al. MELK inhibition in Diffuse Intrinsic Pontine Glioma. Clin Cancer Res. 2018 Jul 30. pii: clincanres.0924.2018. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	1.9088 mL	9.5442 mL	19.0883 mL	47.7209 mL
	5 mM	0.3818 mL	1.9088 mL	3.8177 mL	9.5442 mL
	10 mM	0.1909 mL	0.9544 mL	1.9088 mL	4.7721 mL
DMSO	15 mM	0.1273 mL	0.6363 mL	1.2726 mL	3.1814 mL
	20 mM	0.0954 mL	0.4772 mL	0.9544 mL	2.3860 mL
	25 mM	0.0764 mL	0.3818 mL	0.7635 mL	1.9088 mL
	30 mM	0.0636 mL	0.3181 mL	0.6363 mL	1.5907 mL
	40 mM	0.0477 mL	0.2386 mL	0.4772 mL	1.1930 mL
	50 mM	0.0382 mL	0.1909 mL	0.3818 mL	0.9544 mL
	60 mM	0.0318 mL	0.1591 mL	0.3181 mL	0.7953 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.

OTSSP167 hydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OTSSP1671431698-10-0OTS167OTSSP 167OTSSP-167OTS 167OTS-167MELKMaternal embryonic leucine zipper kinaseInhibitorinhibitorinhibit

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OTSSP167 hydrochloride (Synonyms: OTS167 hydrochloride)

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OTSSP167 hydrochloride Related Antibodies

19 Publications Citing Use of MCE OTSSP167 hydrochloride

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