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製品番号: HY-187930

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HPK1-IN-72

HPK1-IN-72 is an orally active and selective HPK1/MAP4K1 inhibitor with an IC₅₀ of 52.4 nM against human targets. HPK1-IN-72 inhibits HPK1 activation, blocks the negative regulation of T cell receptor signaling, restores T cell receptor signal transduction and enhances T cell function. HPK1-IN-72 suppresses tumor growth, exhibits potent single-agent anti-tumor efficacy, and also produces synergistic effects with anti-PD-1 antibodies or anti-PD-L1/IL-15 immunocytokine prodrugs. HPK1-IN-72 can be used in research related to breast cancer, colorectal cancer and prostate cancer.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2965385-11-7
分子式: C₂₅H₂₆N₄O₄S
分子量:478.56

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (282 KB)

HPK1-IN-72 構造式

CAS 番号: 2965385-11-7

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

HPK1

52.4 nM (IC₅₀)

MAP4K アイソフォーム固有の製品をすべて表示 :

体外実験

OthersAdaptive ImmunityCytokines & Chemokines

Others

HPK1-IN-72 (compound 23) potently inhibits purified HPK1 kinase, with an IC₅₀ of 52.4 nM; it exhibits 20- to 190-fold higher selectivity for HPK1 over the MAP4K family kinases GCK, GLK and HGK, with a selectivity of over 190-fold against GLK; when tested against a kinome panel consisting of 109 human kinases, it inhibits HPK1 and four additional kinases (VEGFR3, RET, CSF1R, KHS) by more than 90%^[1].

Adaptive Immunity

HPK1-IN-72 (0.1-1 μM; 2 h) inhibits the phosphorylation of SLP-76 in Jurkat T cells and primary mouse T cells, confirming its ability to inhibit HPK1 at the cellular level^[1].

Adaptive Immunity

Cytokines & Chemokines

HPK1-IN-72 (0.1-1 μM; 24 h) dose-dependently enhances NFAT-driven luciferase activity in Jurkat-Lucia NFAT reporter cells co-stimulated with PMA (HY-18739) and Ionomycin (HY-13434), thereby potentiating the TCR signaling pathway^[1].
HPK1-IN-72 (0.1-1 μM; 24-72 h) increases IL-2 secretion levels in wild-type Jurkat T cells and primary mouse splenocytes via specific inhibition of HPK1; enhances antigen-specific IFN-γ secretion in OT-1 CD8⁺ T cells stimulated with OVA peptide; and reverses the immunosuppression induced by PGE2 and NECA (HY-103173) by promoting IFN-γ secretion in human primary T cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Jurkat T cells, primary mouse T cells
Concentration:

0.1, 0.3, 1 μM
Incubation Time:

2 h
Result:

Effectively inhibited phosphorylation of SLP-76 in both Jurkat T cells and primary mouse T cells after anti-CD3 stimulation.

ELISA Assay^[1]

Cell Line:

wild-type Jurkat T cells, HPK1-knockout Jurkat T cells, primary mouse splenocytes
Concentration:

0.1, 0.3, 1 μM
Incubation Time:

24 h (Jurkat cells)
72 h (mouse splenocytes)
Result:

Significantly increased IL-2 secretion in wild-type Jurkat T cells and primary mouse splenocytes compared to stimulated controls.
No enhancement of IL-2 secretion was observed in HPK1-knockout Jurkat T cells, confirming target specificity.
A bell-shaped dose-response curve was observed at higher concentrations.

ELISA Assay^[1]

Cell Line:

OT-1 antigen-specific CD8+ T cells
Concentration:

0.1, 0.3, 1 μM
Incubation Time:

72 h
Result:

Significantly increased IFN-γ secretion in OVA peptide-stimulated OT-1 CD8⁺ T cells.

ELISA Assay^[1]

Cell Line:

human primary T cells
Concentration:

1 μM
Incubation Time:

72 h
Result:

Nearly reversed the immunosuppressive effect of PGE2 and NECA, significantly increasing IFN-γ secretion in human primary T cells.

Parmacokinetics

Species	Dose	Route	AUC_0-∞	CL	V_z	F	T_1/2	T_max	C_max
Mice^[1]	1 mg/kg	i.v.	725 ng·h/mL	1427 mL/h/kg	2695 mL/kg	31.6 %	/	/	/
Mice^[1]	3 mg/kg	p.o.	688 ng·h/mL	/	/	/	3.90 h	0.278 h	313 ng/mL

体内実験

Anti-cancerImmune Tolerance & Immunosuppression

Anti-cancer

HPK1-IN-72 (compound 23) (27-50 mg/kg; p.o.; once daily; for 17 consecutive days) dose-dependently inhibits the growth of 4T1 breast cancer tumors in Balb/c mice^[1].

Anti-cancer

Immune Tolerance & Immunosuppression

HPK1‑IN‑72 (50 mg/kg; p.o.; once daily; for 11 consecutive days) shows only moderate activity against CT26 colon tumors in Balb/c mice, but combination treatment with anti‑PD‑1 antibody exerts a synergistic effect to enhance anti‑tumor efficacy^[1].
HPK1‑IN‑72 (50 mg/kg; p.o.; once daily; for 7 consecutive days) inhibits the growth of RM‑1 prostate tumors in C57BL/6J mice, and exerts a synergistic effect when combined with P‑T‑MMP^[1].

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

Animal Model:

Balb/c (8-10 weeks old, subcutaneous implantation of 4T1 cells (3 × 10⁵ cells))^[1]
Dosage:

27 mg/kg; 50 mg/kg
Administration:

p.o.; daily; 17 days
Result:

Achieved tumor growth inhibition (TGI) rate of 40.9% at 27 mg/kg.
Achieved tumor growth inhibition (TGI) rate of 57.9% at 50 mg/kg.

Animal Model:

Balb/c (8-10 weeks old, subcutaneous implantation of CT26 cells (2.5 × 10⁵ cells))^[1]
Dosage:

50 mg/kg
Administration:

p.o.; daily; 11 days
Result:

Exhibited modest antitumor activity as monotherapy.
Produced marked tumor suppression superior to either monotherapy alone when combined with an anti-PD-1 antibody.

Animal Model:

C57BL/6J (8-10 weeks old, subcutaneous implantation of RM-1 cells (5 × 10⁵ cells))^[1]
Dosage:

50 mg/kg
Administration:

p.o.; daily; 7 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 52.3% as monotherapy.
Achieved a tumor growth inhibition (TGI) rate of 81.9% when combined with P-T-MMP (anti-PD-L1/IL-15 prodrug).

Related Protocols :

化学情報

CAS 番号 2965385-11-7
分子量 478.56
分子式 C₂₅H₂₆N₄O₄S
SMILES

OC(C)(C#CC1=CC(COC2=CC(C3=NC4=C(S3)CN(CC4)C(CO)=O)=CN=C2N)=CC=C1)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (282 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Wang Y, et al. Discovery of Thiazolo[5,4-c]pyridine Derivatives as Novel Hematopoietic Progenitor Kinase 1 Inhibitors for Tumor Immunotherapy. J Med Chem. 2026 Aug 13;69(15):18739-18763.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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HPK1-IN-72

MAP4K アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC50 & Target

体外実験

Parmacokinetics

体内実験

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

HPK1-IN-72 関連分類

HY-187930 関連分類

Bioz

Keywords

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