Cat. No.: HY-15512A

OTSSP167 hydrochloride

Name: OTSSP167 hydrochloride
Brand: MedChemExpress
SKU: HY-15512A
Price: 100.00 USD
Availability: InStock
Rating: 5 (24 reviews)

(Synonyms: OTS167 hydrochloride)

24 Cited Publications

고객리뷰

Based on 24 publication(s) in Google Scholar

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.78%
CAS No.: 1431698-10-0
화학식: C₂₅H₂₉Cl₃N₄O₂
분자량:523.88

보관:

4°C, sealed storage, away from moisture

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

OTSSP167 hydrochloride Chemical Structure

CAS No.: 1431698-10-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (24)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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.

Chemical Information

CAS No. 1431698-10-0
Appearance Solid
분자량 523.88
화학식 C₂₅H₂₉Cl₃N₄O₂
Color Light yellow to yellow
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
Synonyms

OTS167 hydrochloride
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture

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

Publications (24)

All IPWB

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Journal Impact Factor

Mol Cancer

Maternal embryonic leucine zipper kinase enhances gastric cancer progression via the FAK/Paxillin pathway. [Abstract]

2014 May 4:13:100. PMID: 24885567

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
Nat Cancer

A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance. [Abstract]

2024 Aug;5(8):1250-1266. PMID: 38992135
Blood Cancer J

Maternal embryonic leucine zipper kinase is a novel target for diffuse large B cell lymphoma and mantle cell lymphoma. [Abstract]

2019 Nov 18;9(12):87. PMID: 31740676

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.
Neuro Oncol

MEK/MELK inhibition and blood-brain barrier deficiencies in atypical teratoid/rhabdoid tumors. [Abstract]

2020 Jan 11;22(1):58-69. PMID: 31504799
Clin Cancer Res

MELK Inhibition in Diffuse Intrinsic Pontine Glioma. [Abstract]

2018 Nov 15;24(22):5645-5657. PMID: 30061363

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.
Free Radic Biol Med

Pharmacological inhibition of MELK restricts ferroptosis and the inflammatory response in colitis and colitis-propelled carcinogenesis. [Abstract]

2021 Aug 20:172:312-329. PMID: 34144192
EMBO Mol Med

Identification of potential therapeutic targets in prostate cancer through a cross-species approach. [Abstract]

2018 Mar;10(3):e8274. PMID: 29437778

OTSSP167 hydrochloride purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2018 Mar;10(3):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.
Int J Oncol

Exposure to escalating olaparib does not induce acquired resistance to PARPi and to other chemotherapeutic compounds in ovarian cancer cell lines. [Abstract]

2022 Jul;61(1):89. PMID: 35642662
Eur J Pharmacol

OTSSP167 suppresses TNBC brain metastasis via ROS-driven P38/JNK and FAK/ERK pathways. [Abstract]

2025 Oct 5:1004:178017. PMID: 40744390
Int J Mol Sci

MELK as a Mediator of Stemness and Metastasis in Aggressive Subtypes of Breast Cancer. [Abstract]

2025 Mar 3;26(5):2245. PMID: 40076867
Sci Rep

Zinc finger protein ZPR9 functions as an activator of AMPK-related serine/threonine kinase MPK38/MELK involved in ASK1/TGF-β/p53 signaling pathways. [Abstract]

2017 Feb 14:7:42502. PMID: 28195154

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
Gynecol Oncol

MELK expression in ovarian cancer correlates with poor outcome and its inhibition by OTSSP167 abrogates proliferation and viability of ovarian cancer cells. [Abstract]

2017 Apr;145(1):159-166. PMID: 28214016

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).
FEBS J

Nemo-like kinase modulates glucocorticoid-induced erythroid progenitor differentiation by regulating stability of the glucocorticoid receptor. [Abstract]

2026 Feb 2. PMID: 41629744
Adv Ther (Weinh)

2025 Oct 24.
PLoS One

Genome-wide effects of MELK-inhibitor in triple-negative breast cancer cells indicate context-dependent response with p53 as a key determinant. [Abstract]

2017 Feb 24;12(2):e0172832. PMID: 28235006

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.
Biochem Biophys Res Commun

The crystal structure of MPK38 in complex with OTSSP167, an orally administrative MELK selective inhibitor. [Abstract]

2014 Apr 25;447(1):7-11. PMID: 24657156
University of Michigan

2026.
bioRxiv

2026 Apr 24.
University of Washington

2025.
Elife

MELK expression correlates with tumor mitotic activity but is not required for cancer growth. [Abstract]

2018 Feb 8:7:e32838. PMID: 29417930
Oncotarget

MELK is a novel therapeutic target in high-risk neuroblastoma. [Abstract]

2017 Dec 20;9(2):2591-2602. PMID: 29416794

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.
Elife

CRISPR/Cas9 mutagenesis invalidates a putative cancer dependency targeted in on-going clinical trials. [Abstract]

2017 Mar 24:6:e24179. PMID: 28337968
Patent

US20160291017A1.

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.
Oncotarget

Maternal embryonic leucine zipper kinase serves as a poor prognosis marker and therapeutic target in gastric cancer. [Abstract]

2016 Feb 2;7(5):6266-80. PMID: 26701722

용액&용해도

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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.

Bioz

Keywords

OTSSP167 hydrochloride

24 Cited Publications

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OTSSP167 hydrochloride

Publications Citing Use of MedChemExpress (MCE) OTSSP167 hydrochloride